edoc

Browse by Basel Contributors ID

Up a level
Export as [feed] Atom [feed] RSS 1.0 [feed] RSS 2.0
Group by: Date | Item Type | Refereed | No Grouping
Jump to: 2023 | 2022 | 2021 | 2020 | 2019 | 2018 | 2017 | 2016 | 2015 | 2014 | 2013 | 2012 | 2011 | 2010 | 2009

2023

Imlay, L. S. and Lawong, A. K. and Gahalawat, S. and Kumar, A. and Xing, C. and Mittal, N. and Wittlin, S. and Churchyard, A. and Niederstrasser, H. and Crespo-Fernandez, B. and Posner, B. A. and Gamo, F. J. and Baum, J. and Winzeler, E. A. and Laleu, B. and Ready, J. M. and Phillips, M. A.. (2023) Fast-killing tyrosine amide ((S)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance locus (PfCARL). ACS Infect Dis, 9 (3). pp. 527-539.

Nguyen, W. and Dans, M. G. and Currie, I. and Awalt, J. K. and Bailey, B. L. and Lumb, C. and Ngo, A. and Favuzza, P. and Palandri, J. and Ramesh, S. and Penington, J. and Jarman, K. E. and Mukherjee, P. and Chakraborty, A. and Maier, A. G. and van Dooren, G. G. and Papenfuss, T. and Wittlin, S. and Churchyard, A. and Baum, J. and Winzeler, E. A. and Baud, D. and Brand, S. and Jackson, P. F. and Cowman, A. F. and Sleebs, B. E.. (2023) 7-N-substituted-3-oxadiazole quinolones with potent antimalarial activity target the cytochrome bc1 complex. ACS Infect Dis, 9 (3). pp. 668-691.

Walz, A. and Duffey, M. and Aljayyoussi, G. and Sax, S. and Leroy, D. and Besson, A. and Burrows, J. N. and Cherkaoui-Rbati, M. H. and Gobeau, N. and Westwood, M.-A. and Siethoff, C. and Gamo, S. and Mäser, P. and Wittlin, S.. (2023) The Parasite Reduction Ratio (PRR) assay version 2: standardized assessment of Plasmodium falciparum viability after antimalarial treatment in vitro. Pharmaceuticals (Basel), 16 (2). p. 163.

Davies, H. and Bergmann, B. and Walloch, P. and Nerlich, C. and Hansen, C. and Wittlin, S. and Spielmann, T. and Treeck, M. and Beitz, E.. (2023) The plasmodium lactate/H+ transporter PfFNT is essential and druggable in vivo. Antimicrob Agents Chemother, 67 (8). e0035623.

2022

de Vries, L. E. and Jansen, P. A. M. and Barcelo, C. and Munro, J. and Verhoef, J. M. J. and Pasaje, C. F. A. and Rubiano, K. and Striepen, J. and Abla, N. and Berning, L. and Bolscher, J. M. and Demarta-Gatsi, C. and Henderson, R. W. M. and Huijs, T. and Koolen, K. M. J. and Tumwebaze, P. K. and Yeo, T. and Aguiar, A. C. C. and Angulo-Barturen, I. and Churchyard, A. and Baum, J. and Fernandez, B. C. and Fuchs, A. and Gamo, F. J. and Guido, R. V. C. and Jimenez-Diaz, M. B. and Pereira, D. B. and Rochford, R. and Roesch, C. and Sanz, L. M. and Trevitt, G. and Witkowski, B. and Wittlin, S. and Cooper, R. A. and Rosenthal, P. J. and Sauerwein, R. W. and Schalkwijk, J. and Hermkens, P. H. H. and Bonnert, R. V. and Campo, B. and Fidock, D. A. and Llinas, M. and Niles, J. C. and Kooij, T. W. A. and Dechering, K. J.. (2022) Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183. Nat Commun, 13. p. 2158.

Dong, Y. and Sonawane, Y. and Maher, S. P. and Zeeman, A. M. and Chaumeau, V. and Vantaux, A. and Cooper, C. A. and Chiu, F. C. K. and Ryan, E. and McLaren, J. and Chen, G. and Wittlin, S. and Witkowski, B. and Nosten, F. and Sriraghavan, K. and Kyle, D. E. and Kocken, C. H. M. and Charman, S. A. and Vennerstrom, J. L.. (2022) Metabolic, pharmacokinetic, and activity profile of the liver stage antimalarial (RC-12). ACS Omega, 7 (14). pp. 12401-12411.

Laleu, B. and Rubiano, K. and Yeo, T. and Hallyburton, I. and Anderson, M. and Crespo-Fernandez, B. and Gamo, F. J. and Antonova-Koch, Y. and Orjuela-Sanchez, P. and Wittlin, S. and Jana, G. P. and Maity, B. C. and Chenu, E. and Duffy, J. and Sjo, P. and Waterson, D. and Winzeler, E. and Guantai, E. and Fidock, D. A. and Hansson, T.. (2022) Exploring a tetrahydroquinoline antimalarial hit from the medicines for malaria pathogen box and the identification of its mode of resistance as PfeEF2. ChemMedChem, 17 (22). e202200393.

Lowe, M. A. and Cardenas, A. and Valentin, J. P. and Zhu, Z. and Abendroth, J. and Castro, J. L. and Class, R. and Delaunois, A. and Fleurance, R. and Gerets, H. and Gryshkova, V. and King, L. and Lorimer, D. D. and MacCoss, M. and Rowley, J. H. and Rosseels, M. L. and Royer, L. and Taylor, R. D. and Wong, M. and Zaccheo, O. and Chavan, V. P. and Ghule, G. A. and Tapkir, B. K. and Burrows, J. N. and Duffey, M. and Rottmann, M. and Wittlin, S. and Angulo-Barturen, I. and Jiménez-Díaz, M. B. and Striepen, J. and Fairhurst, K. J. and Yeo, T. and Fidock, D. A. and Cowman, A. F. and Favuzza, P. and Crespo-Fernandez, B. and Gamo, F. J. and Goldberg, D. E. and Soldati-Favre, D. and Laleu, B. and de Haro, T.. (2022) Discovery and characterization of potent, efficacious, orally available antimalarial plasmepsin X inhibitors and preclinical safety assessment of UCB7362. Journal of medicinal chemistry, 65 (20). pp. 14121-14143.

Xie, S. C. and Metcalfe, R. D. and Dunn, E. and Morton, C. J. and Huang, S. C. and Puhalovich, T. and Du, Y. and Wittlin, S. and Nie, S. and Luth, M. R. and Ma, L. and Kim, M. S. and Pasaje, C. F. A. and Kumpornsin, K. and Giannangelo, C. and Houghton, F. J. and Churchyard, A. and Famodimu, M. T. and Barry, D. C. and Gillett, D. L. and Dey, S. and Kosasih, C. C. and Newman, W. and Niles, J. C. and Lee, M. C. S. and Baum, J. and Ottilie, S. and Winzeler, E. A. and Creek, D. J. and Williamson, N. and Parker, M. W. and Brand, S. and Langston, S. P. and Dick, L. R. and Griffin, M. D. W. and Gould, A. E. and Tilley, L.. (2022) Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy. Science, 376 (6597). pp. 1074-1079.

Mambwe, D. and Korkor, CM. and Mabhula, A. and Ngqumba, Z. and Cloete, C. and Kumar, M. and Barros, PL. and Leshabane, M. and Coertzen, D. and Taylor, D. and Gibhard, L. and Njoroge, M. and Lawrence, N. and Reader, J. and Moreira, DR. and Birkholtz, LM. and Wittlin, S. and Egan, TJ. and Chibale, K.. (2022) Novel 3-trifluoromethyl-1,2,4-oxadiazole analogues of astemizole with multi-stage antiplasmodium activity and; in vivo; efficacy in a; Plasmodium berghei; mouse malaria infection model. Journal of medicinal chemistry, 65 (24). pp. 16695-16715.

2021

Cheuka, P. M. and Centani, L. and Arendse, L. B. and Fienberg, S. and Wambua, L. and Renga, S. S. and Dziwornu, G. A. and Kumar, M. and Lawrence, N. and Taylor, D. and Wittlin, S. and Coertzen, D. and Reader, J. and van der Watt, M. and Birkholtz, L. M. and Chibale, K.. (2021) New amidated 3,6-diphenylated imidazopyridazines with potent antiplasmodium activity are dual inhibitors of; Plasmodium; phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. ACS Infect Dis, 7 (1). pp. 34-46.

Boss, C. and Wittlin, S.. (2021) Our exciting journey to ACT-451840. Chimia, 75 (11). pp. 916-922.

Dziwornu, G. A. and Coertzen, D. and Leshabane, M. and Korkor, C. M. and Cloete, C. K. and Njoroge, M. and Gibhard, L. and Lawrence, N. and Reader, J. and van der Watt, M. and Wittlin, S. and Birkholtz, L. M. and Chibale, K.. (2021) Antimalarial benzimidazole derivatives incorporating phenolic mannich base side chains inhibit microtubule and hemozoin formation: structure-activity relationship and in vivo oral efficacy studies. Journal of medicinal chemistry, 64 (8). pp. 5198-5215.

Hitz, E. and Wiedemar, N. and Passecker, A. and Graça, B. A. S. and Scheurer, C. and Wittlin, S. and Brancucci, N. M. B. and Vakonakis, I. and Mäser, P. and Voss, T. S.. (2021) The 3-phosphoinositide-dependent protein kinase 1 is an essential upstream activator of protein kinase A in malaria parasites. PLoS Biol, 19 (12). e3001483.

Hitz, E. and Grüninger, O. and Passecker, A. and Wyss, M. and Scheurer, C. and Wittlin, S. and Beck, H. P. and Brancucci, N. M. B. and Voss, T. S.. (2021) The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis. Commun Biol, 4 (1). p. 336.

Leas, D. A. and Sanford, A. G. and Wu, J. and Cal, M. and Kaiser, M. and Wittlin, S. and Hemsley, R. M. and Darner, E. B. and Lui, L. M. and Davis, P. H. and Vennerstrom, J. L.. (2021) Diaryl ureas as an antiprotozoal chemotype. ACS Infect Dis, 7 (6). pp. 1578-1583.

Le Manach, C. and Dam, J. and Woodland, J. G. and Kaur, G. and Khonde, L. P. and Brunschwig, C. and Njoroge, M. and Wicht, K. J. and Horatscheck, A. and Paquet, T. and Boyle, G. A. and Gibhard, L. and Taylor, D. and Lawrence, N. and Yeo, T. and Mok, S. and Eastman, R. T. and Dorjsuren, D. and Talley, D. C. and Guo, H. and Simeonov, A. and Reader, J. and van der Watt, M. and Erlank, E. and Venter, N. and Zawada, J. W. and Aswat, A. and Nardini, L. and Coetzer, T. L. and Lauterbach, S. B. and Bezuidenhout, B. C. and Theron, A. and Mancama, D. and Koekemoer, L. L. and Birkholtz, L. M. and Wittlin, S. and Delves, M. and Ottilie, S. and Winzeler, E. A. and von Geldern, T. W. and Smith, D. and Fidock, D. A. and Street, L. J. and Basarab, G. S. and Duffy, J. and Chibale, K.. (2021) Identification and profiling of a novel diazaspiro[3.4]octane chemical series active against multiple stages of the human malaria parasite Plasmodium falciparum and optimization efforts. Journal of medicinal chemistry, 64 (4). pp. 2291-2309.

Lawong, A. and Gahalawat, S. and Okombo, J. and Striepen, J. and Yeo, T. and Mok, S. and Deni, I. and Bridgford, J. L. and Niederstrasser, H. and Zhou, A. and Posner, B. and Wittlin, S. and Gamo, F. J. and Crespo, B. and Churchyard, A. and Baum, J. and Mittal, N. and Winzeler, E. and Laleu, B. and Palmer, M. J. and Charman, S. A. and Fidock, D. A. and Ready, J. M. and Phillips, M. A.. (2021) Novel antimalarial tetrazoles and amides active against the hemoglobin degradation pathway in Plasmodium falciparum. Journal of medicinal chemistry, 64 (5). pp. 2739-2761.

Laleu, B. and Akao, Y. and Ochida, A. and Duffy, S. and Lucantoni, L. and Shackleford, D. M. and Chen, G. and Katneni, K. and Chiu, F. C. K. and White, K. L. and Chen, X. and Sturm, A. and Dechering, K. J. and Crespo, B. and Sanz, L. M. and Wang, B. and Wittlin, S. and Charman, S. A. and Avery, V. M. and Cho, N. and Kamaura, M.. (2021) Discovery and structure-activity relationships of quinazolinone-2-carboxamide derivatives as novel orally efficacious antimalarials. Journal of medicinal chemistry, 64 (17). pp. 12582-12602.

Knaab, T. C. and Held, J. and Burckhardt, B. B. and Rubiano, K. and Okombo, J. and Yeo, T. and Mok, S. and Uhlemann, A. C. and Lungerich, B. and Fischli, C. and Pessanha de Carvalho, L. and Mordmüller, B. and Wittlin, S. and Fidock, D. A. and Kurz, T.. (2021) 3-Hydroxy-propanamidines, a new class of orally active antimalarials targeting Plasmodium falciparum. Journal of medicinal chemistry, 64 (6). pp. 3035-3047.

Murithi, J. M. and Pascal, C. and Bath, J. and Boulenc, X. and Gnadig, N. F. and Pasaje, C. F. A. and Rubiano, K. and Yeo, T. and Mok, S. and Klieber, S. and Desert, P. and Jimenez-Diaz, M. B. and Marfurt, J. and Rouillier, M. and Cherkaoui-Rbati, M. H. and Gobeau, N. and Wittlin, S. and Uhlemann, A. C. and Price, R. N. and Wirjanata, G. and Noviyanti, R. and Tumwebaze, P. and Cooper, R. A. and Rosenthal, P. J. and Sanz, L. M. and Gamo, F. J. and Joseph, J. and Singh, S. and Bashyam, S. and Augereau, J. M. and Giraud, E. and Bozec, T. and Vermat, T. and Tuffal, G. and Guillon, J. M. and Menegotto, J. and Salle, L. and Louit, G. and Cabanis, M. J. and Nicolas, M. F. and Doubovetzky, M. and Merino, R. and Bessila, N. and Angulo-Barturen, I. and Baud, D. and Bebrevska, L. and Escudie, F. and Niles, J. C. and Blasco, B. and Campbell, S. and Courtemanche, G. and Fraisse, L. and Pellet, A. and Fidock, D. A. and Leroy, D.. (2021) The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance. Sci Transl Med, 13 (603). eabg6013.

Palmer, M. J. and Deng, X. and Watts, S. and Krilov, G. and Gerasyuto, A. and Kokkonda, S. and El Mazouni, F. and White, J. and White, K. L. and Striepen, J. and Bath, J. and Schindler, K. A. and Yeo, T. and Shackleford, D. M. and Mok, S. and Deni, I. and Lawong, A. and Huang, A. and Chen, G. and Wang, W. and Jayaseelan, J. and Katneni, K. and Patil, R. and Saunders, J. and Shahi, S. P. and Chittimalla, R. and Angulo-Barturen, I. and Jimenez-Diaz, M. B. and Wittlin, S. and Tumwebaze, P. K. and Rosenthal, P. J. and Cooper, R. A. and Aguiar, A. C. C. and Guido, R. V. C. and Pereira, D. B. and Mittal, N. and Winzeler, E. A. and Tomchick, D. R. and Laleu, B. and Burrows, J. N. and Rathod, P. K. and Fidock, D. A. and Charman, S. A. and Phillips, M. A.. (2021) Potent antimalarials with development potential identified by structure-guided computational optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series. Journal of medicinal chemistry, 64 (9). pp. 6085-6136.

Okaniwa, M. and Shibata, A. and Ochida, A. and Akao, Y. and White, K. L. and Shackleford, D. M. and Duffy, S. and Lucantoni, L. and Dey, S. and Striepen, J. and Yeo, T. and Mok, S. and Aguiar, A. C. C. and Sturm, A. and Crespo, B. and Sanz, L. M. and Churchyard, A. and Baum, J. and Pereira, D. B. and Guido, R. V. C. and Dechering, K. J. and Wittlin, S. and Uhlemann, A. C. and Fidock, D. A. and Niles, J. C. and Avery, V. M. and Charman, S. A. and Laleu, B.. (2021) Repositioning and characterization of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives as Plasmodium cytoplasmic prolyl-trna synthetase inhibitors. ACS Infect Dis, 7 (6). pp. 1680-1689.

Shackleford, D. M. and Chiu, F. C. K. and Katneni, K. and Blundell, S. and McLaren, J. and Wang, X. and Zhou, L. and Sriraghavan, K. and Alker, A. M. and Hunziker, D. and Scheurer, C. and Zhao, Q. and Dong, Y. and Mohrle, J. J. and Abla, N. and Matile, H. and Wittlin, S. and Vennerstrom, J. L. and Charman, S. A.. (2021) Cytochrome P450-mediated metabolism and CYP Inhibition for the synthetic peroxide antimalarial OZ439. ACS Infect Dis, 7 (7). pp. 1885-1893.

Xie, S. C. and Metcalfe, R. D. and Mizutani, H. and Puhalovich, T. and Hanssen, E. and Morton, C. J. and Du, Y. and Dogovski, C. and Huang, S. C. and Ciavarri, J. and Hales, P. and Griffin, R. J. and Cohen, L. H. and Chuang, B. C. and Wittlin, S. and Deni, I. and Yeo, T. and Ward, K. E. and Barry, D. C. and Liu, B. and Gillett, D. L. and Crespo-Fernandez, B. F. and Ottilie, S. and Mittal, N. and Churchyard, A. and Ferguson, D. and Aguiar, A. C. C. and Guido, R. V. C. and Baum, J. and Hanson, K. K. and Winzeler, E. A. and Gamo, F. J. and Fidock, D. A. and Baud, D. and Parker, M. W. and Brand, S. and Dick, L. R. and Griffin, M. D. W. and Gould, A. E. and Tilley, L.. (2021) Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome. Proc Natl Acad Sci U S A, 118 (39). e2107213118.

Wittlin, S. and Mäser, P.. (2021) From magic bullet to magic bomb: reductive bioactivation of antiparasitic agents. ACS Infect Dis, 7 (10). pp. 2777-2786.

2020

Ahenkorah, S. and Coertzen, D. and Tong, J. X. and Fridianto, K. and Wittlin, S. and Birkholtz, L. M. and Tan, K. S. W. and Lam, Y. and Go, M. L. and Haynes, R. K.. (2020) Antimalarial N1,N3-dialkyldioxonaphthoimidazoliums: synthesis, biological activity, and structure-activity relationships. ACS medicinal chemistry letters, 11. pp. 49-55.

Burgert, Lydia and Rottmann, Matthias and Wittlin, Sergio and Gobeau, Nathalie and Krause, Andreas and Dingemanse, Jasper and Möhrle, Jörg J. and Penny, Melissa A.. (2020) Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development. Scientific reports, 10. p. 4410.

Kokkonda, Sreekanth and Deng, Xiaoyi and White, Karen L. and El Mazouni, Farah and White, John and Shackleford, David M. and Katneni, Kasiram and Chiu, Francis C. K. and Barker, Helena and McLaren, Jenna and Crighton, Elly and Chen, Gong and Angulo-Barturen, Inigo and Jimenez-Diaz, Maria Belen and Ferrer, Santiago and Huertas-Valentin, Leticia and Martinez-Martinez, Maria Santos and Lafuente-Monasterio, Maria Jose and Chittimalla, Rajesh and Shahi, Shatrughan P. and Wittlin, Sergio and Waterson, David and Burrows, Jeremy N. and Matthews, Dave and Tomchick, Diana and Rathod, Pradipsinh K. and Palmer, Michael J. and Charman, Susan A. and Phillips, Margaret A.. (2020) Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria. Journal of medicinal chemistry, 63 (9). pp. 4929-4956.

Horatscheck, A. and Andrijevic, A. and Nchinda, A. T. and Le Manach, C. and Paquet, T. and Khonde, L. P. and Dam, J. and Pawar, K. and Taylor, D. and Lawrence, N. and Brunschwig, C. and Gibhard, L. and Njoroge, M. and Reader, J. and van der Watt, M. and Wicht, K. and de Sousa, A. C. C. and Okombo, J. and Maepa, K. and Egan, T. J. and Birkholtz, L. M. and Basarab, G. S. and Wittlin, S. and Fish, P. V. and Street, L. J. and Duffy, J. and Chibale, K.. (2020) Identification of 2,4-disubstituted imidazopyridines as hemozoin formation inhibitors with fast-killing kinetics and in vivo efficacy in the Plasmodium falciparum NSG mouse model. Journal of medicinal chemistry, 63 (21). pp. 13013-13030.

Potluri, V. and Shandil, R. K. and Gavara, R. and Sambasivam, G. and Campo, B. and Wittlin, S. and Narayanan, S.. (2020) Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J, 19. p. 365.

2019

Gilson, Paul R. and Nguyen, William and Poole, William A. and Teixeira, Jose E. and Thompson, Jennifer K. and Guo, Kaiyuan and Stewart, Rebecca J. and Ashton, Trent D. and White, Karen L. and Sanz, Laura M. and Gamo, Francisco-Javier and Charman, Susan A. and Wittlin, Sergio and Duffy, James and Tonkin, Christopher J. and Tham, Wai-Hong and Crabb, Brendan S. and Cooke, Brian M. and Huston, Christopher D. and Cowman, Alan F. and Sleebs, Brad E.. (2019) Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Evaluation of 4-amino 2-anilinoquinazolines against Plasmodium and other apicomplexan parasites in vitro and in a P. falciparum humanized NOD-scid IL2Rynull mouse model of malaria. Antimicrobial agents and chemotherapy, 63 (3). e01804-18.

Kumar, Malkeet and Okombo, John and Mambwe, Dickson and Taylor, Dale and Lawrence, Nina and Reader, Janette and van der Watt, Mariëtte and Fontinha, Diana and Sanches-Vaz, Margarida and Bezuidenhout, Belinda C. and Lauterbach, Sonja B. and Liebenberg, Dale and Birkholtz, Lyn-Marie and Coetzer, Theresa L. and Prudêncio, Miguel and Egan, Timothy J. and Wittlin, Sergio and Chibale, Kelly. (2019) Multistage antiplasmodium activity of astemizole analogues and inhibition of hemozoin formation as a contributor to their mode of action. ACS infectious diseases, 5 (2). pp. 303-315.

Mayoka, Godfrey and Njoroge, Mathew and Okombo, John and Gibhard, Liezl and Sanches-Vaz, Margarida and Fontinha, Diana and Birkholtz, Lyn-Marie and Reader, Janette and van der Watt, Mariëtte and Coetzer, Theresa L. and Lauterbach, Sonja and Churchyard, Alisje and Bezuidenhout, Belinda and Egan, Timothy J. and Yeates, Clive Leonard and Wittlin, Sergio and Prudêncio, Miguel and Chibale, Kelly. (2019) Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria. Journal of medicinal chemistry, 62 (2). pp. 1022-1035.

Okombo, John and Brunschwig, Christel and Singh, Kawaljit and Dziwornu, Godwin Akpeko and Barnard, Linley and Njoroge, Mathew and Wittlin, Sergio and Chibale, Kelly. (2019) Antimalarial pyrido[1,2-a]benzimidazole derivatives with mannich base side chains: synthesis, pharmacological evaluation and reactive metabolite trapping studies. ACS infectious diseases, 5 (3). pp. 372-384.

Hooft van Huijsduijnen, R. and Wells, T. and Tanner, M. and Wittlin, S.. (2019) Two successful decades of Swiss collaborations to develop new anti-malarials. Malaria journal, 18. p. 94.

Attram, H. D. and Wittlin, S. and Chibale, K.. (2019) Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. MedChemComm , 10 (3). pp. 450-455.

Baragaña, Beatriz and Forte, Barbara and Choi, Ryan and Nakazawa Hewitt, Stephen and Bueren-Calabuig, Juan A. and Pisco, João Pedro and Peet, Caroline and Dranow, David M. and Robinson, David A. and Jansen, Chimed and Norcross, Neil R. and Vinayak, Sumiti and Anderson, Mark and Brooks, Carrie F. and Cooper, Caitlin A. and Damerow, Sebastian and Delves, Michael and Dowers, Karen and Duffy, James and Edwards, Thomas E. and Hallyburton, Irene and Horst, Benjamin G. and Hulverson, Matthew A. and Ferguson, Liam and Jiménez-Díaz, María Belén and Jumani, Rajiv S. and Lorimer, Donald D. and Love, Melissa S. and Maher, Steven and Matthews, Holly and McNamara, Case W. and Miller, Peter and O'Neill, Sandra and Ojo, Kayode K. and Osuna-Cabello, Maria and Pinto, Erika and Post, John and Riley, Jennifer and Rottmann, Matthias and Sanz, Laura M. and Scullion, Paul and Sharma, Arvind and Shepherd, Sharon M. and Shishikura, Yoko and Simeons, Frederick R. C. and Stebbins, Erin E. and Stojanovski, Laste and Straschil, Ursula and Tamaki, Fabio K. and Tamjar, Jevgenia and Torrie, Leah S. and Vantaux, Amélie and Witkowski, Benoît and Wittlin, Sergio and Yogavel, Manickam and Zuccotto, Fabio and Angulo-Barturen, Iñigo and Sinden, Robert and Baum, Jake and Gamo, Francisco-Javier and Mäser, Pascal and Kyle, Dennis E. and Winzeler, Elizabeth A. and Myler, Peter J. and Wyatt, Paul G. and Floyd, David and Matthews, David and Sharma, Amit and Striepen, Boris and Huston, Christopher D. and Gray, David W. and Fairlamb, Alan H. and Pisliakov, Andrei V. and Walpole, Chris and Read, Kevin D. and Van Voorhis, Wesley C. and Gilbert, Ian H.. (2019) Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proceedings of the National Academy of Sciences of the United States of America, 116 (14). pp. 7015-7020.

Baartzes, N. and Stringer, T. and Seldon, R. and Warner, D. F. and Taylor, D. and Wittlin, S. and Chibale, K. and Smith, G. S.. (2019) Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids : antimicrobial evaluation and mechanistic insights. European journal of medicinal chemistry, 180. pp. 121-133.

Krieg, R. and Jortzik, E. and Goetz, A. A. and Blandin, S. and Wittlin, S. and Elhabiri, M. and Rahbari, M. and Nuryyeva, S. and Voigt, K. and Dahse, H. M. and Brakhage, A. and Beckmann, S. and Quack, T. and Grevelding, C. G. and Pinkerton, A. B. and Schonecker, B. and Burrows, J. and Davioud-Charvet , E. and Rahlfs, S. and Becker, K.. (2019) Author correction: Arylmethylamino steroids as antiparasitic agents. Nature Communications, 10. p. 2997.

Schalkwijk, Joost and Allman, Erik L. and Jansen, Patrick A. M. and de Vries, Laura E. and Verhoef, Julie M. J. and Jackowski, Suzanne and Botman, Peter N. M. and Beuckens-Schortinghuis, Christien A. and Koolen, Karin M. J. and Bolscher, Judith M. and Vos, Martijn W. and Miller, Karen and Reeves, Stacy A. and Pett, Helmi and Trevitt, Graham and Wittlin, Sergio and Scheurer, Christian and Sax, Sibylle and Fischli, Christoph and Angulo-Barturen, Iñigo and Jiménez-Diaz, Mariá Belén and Josling, Gabrielle and Kooij, Taco W. A. and Bonnert, Roger and Campo, Brice and Blaauw, Richard H. and Rutjes, Floris P. J. T. and Sauerwein, Robert W. and Llinás, Manuel and Hermkens, Pedro H. H. and Dechering, Koen J.. (2019) Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum. Science Translational Medicine, 11 (510). eaas9917.

Walz, A. and Leroy, D. and Andenmatten, N. and Mäser, P. and Wittlin, S.. (2019) Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay. Malaria journal, 18. p. 427.

Jourdan, Joëlle and Walz, Annabelle and Matile, Hugues and Schmidt, Alexander and Wu, Jianbo and Wang, Xiaofang and Dong, Yuxiang and Vennerstrom, Jonathan L. and Schmidt, Remo S. and Wittlin, Sergio and Mäser, Pascal. (2019) Stochastic protein alkylation by antimalarial peroxides. ACS Infectious Diseases, 5 (12). pp. 2067-2075.

2018

Brunschwig, Christel and Lawrence, Nina and Taylor, Dale and Abay, Efrem and Njoroge, Mathew and Basarab, Gregory S. and Le Manach, Claire and Paquet, Tanya and Cabrera, Diego Gonzàlez and Nchinda, Aloysius T. and de Kock, Carmen and Wiesner, Lubbe and Denti, Paolo and Waterson, David and Blasco, Benjamin and Leroy, Didier and Witty, Michael J. and Donini, Cristina and Duffy, James and Wittlin, Sergio and White, Karen L. and Charman, Susan A. and Jiménez-Díaz, Maria Belén and Angulo-Barturen, Iñigo and Herreros, Esperanza and Gamo, Francisco Javier and Rochford, Rosemary and Mancama, Dalu and Coetzer, Theresa L. and van der Watt, Mariëtte E. and Reader, Janette and Birkholtz, Lyn-Marie and Marsh, Kennan C. and Solapure, Suresh M. and Burke, John E. and McPhail, Jacob A. and Vanaerschot, Manu and Fidock, David A. and Fish, Paul V. and Siegl, Peter and Smith, Dennis A. and Wirjanata, Grennady and Noviyanti, Rintis and Price, Ric N. and Marfurt, Jutta and Silue, Kigbafori D. and Street, Leslie J. and Chibale, Kelly. (2018) UCT943, a next generation Plasmodium falciparum PI4K inhibitor preclinical candidate for the treatment of malaria. Antimicrobial agents and chemotherapy, 62 (9). e00012-e00018.

Kaur, Gurminder and Pavadai, Elumalai and Wittlin, Sergio and Chibale, Kelly. (2018) 3D-QSAR modeling and synthesis of new fusidic acid derivatives as antiplasmodial agents. Journal of Chemical Information and Modeling, 58 (8). pp. 1553-1560.

Cheuka, P. M. and Larence, N. and Taylor, D. and Wittlin, S. and Chibale, K.. (2018) Antiplasmodial imidazopyridazines : structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles. MedChemComm , 9 (10). pp. 1733-1745.

Grogg, Marcel and Hilvert, Donald and Ebert, Marc-Olivier and Beck, Albert K. and Seebach, Dieter and Kurth, Felix and Dittrich, Petra S. and Sparr, Christof and Wittlin, Sergio and Rottmann, Matthias and Mäser, Pascal. (2018) Cell penetration, herbicidal activity, and in-vivo-toxicity of oligo-arginine derivatives and of novel guanidinium-rich compounds derived from the biopolymer cyanophycin. Helvetica Chimica Acta, 101 (10). e1800112.

Le Manach, Claire and Paquet, Tanya and Wicht, Kathryn and Nchinda, Aloysius T. and Brunschwig, Christel and Njoroge, Mathew and Gibhard, Liezl and Taylor, Dale and Lawrence, Nina and Wittlin, Sergio and Eyermann, Charles J. and Basarab, Gregory S. and Duffy, James and Fish, Paul V. and Street, Leslie J. and Chibale, Kelly. (2018) Antimalarial lead-optimization studies on a 2,6-imidazopyridine series within a constrained chemical space to circumvent atypical dose-response curves against multidrug resistant parasite strains. Journal of medicinal chemistry, 61 (20). pp. 9371-9385.

Brunschwig, C. Lawrence and N. Taylor, D. Abay and E. Njoroge, M. Basarab and G. S. Le Manach, C. Paquet and T. Gonzalez Cabrera, D. Nchinda and A. T. de Kock, C. Wiesner and L. Denti, P. Waterson and D. Blasco, B. Leroy and D. Witty, M. J. Donini and C. Duffy, J. Wittlin and S. White, K. L. Charman and S. A. Jimenez-Diaz, M. B. Angulo-Barturen and I. Herreros, E. Gamo and F. J. Rochford, R. Mancama and D. Coetzer, T. L. van der Watt and M. E. Reader, J. Birkholtz and L. M. Marsh, K. C. Solapure and S. M. Burke, J. E. McPhail and J. A. Vanaerschot, M. Fidock and D. A. Fish, P. V. Siegl and P. Smith, D. A. Wirjanata and G. Noviyanti, R. Price and R. N. Marfurt, J. Silue and K. D. Street, L. J. Chibale. (2018) Erratum for Brunschwig et al., "UCT943, a next-generation Plasmodium falciparum PI4K Inhibitor rreclinical candidate for the treatment of malaria". Antimicrobial agents and chemotherapy, 62 (11). e01941-18.

Gibhard, Liezl and Njoroge, Mathew and Paquet, Tanya and Brunschwig, Christel and Taylor, Dale and Lawrence, Nina and Abay, Efrem and Wittlin, Sergio and Wiesner, Lubbe and Street, Leslie J. and Chibale, Kelly and Basarab, Gregory S.. (2018) Investigating sulfoxide to sulfone conversion as a prodrug strategy for a PI4K inhibitor in a humanized mouse model of malaria. Antimicrobial agents and chemotherapy, 62 (12). e00261-18.

Nchinda, Aloysius T. and Le Manach, Claire and Paquet, Tanya and Gonzàlez Cabrera, Diego and Wicht, Kathryn J. and Brunschwig, Christel and Njoroge, Mathew and Abay, Efrem and Taylor, Dale and Lawrence, Nina and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Lafuente-Monasterio, Maria Jose and Duffy, James and Burrows, Jeremy and Street, Leslie J. and Chibale, Kelly. (2018) Identification of fast-acting 2,6-disubstituted imidazopyridines that are efficacious in the In Vivo humanized Plasmodium falciparum nodscidil2rgamma (null) mouse model of malaria. Journal of medicinal chemistry, 61 (9). pp. 4213-4227.

Boss, C. and Wittlin, S.. (2018) Recent trends in malaria research. In: 2018 Medicinal chemistry reviews: from the medicinal chemistry division of the ACS, 53. Minneapolis, pp. 293-311.

2017

Espinoza-Moraga, Marlene and Singh, Kawaljit and Njoroge, Mathew and Kaur, Gurminder and Okombo, John and De Kock, Carmen and Smith, Peter J. and Wittlin, Sergio and Chibale, Kelly. (2017) Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. Bioorganic & medicinal chemistry, 27 (3). pp. 658-661.

Xu, Ze-Jun and Wittlin, Sergio and Wu, Yikang. (2017) Probing the peroxycarbenium [3+2] cycloaddition reactions with 1,2-disubstituted ethylenes: results and insights. Chemistry (Weinheim an der Bergstrasse, Germany), 23 (9). pp. 2031-2034.

Baumgärtner, Fabian and Jourdan, Joëlle and Scheurer, Christian and Blasco, Benjamin and Campo, Brice and Mäser, Pascal and Wittlin, Sergio. (2017) In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate. Malaria journal, 16. p. 45.

Krieg, Reimar and Jortzik, Esther and Goetz, Alice-Anne and Blandin, Stéphanie and Wittlin, Sergio and Elhabiri, Mourad and Rahbari, Mahsa and Nuryyeva, Selbi and Voigt, Kerstin and Dahse, Hans-Martin and Brakhage, Axel and Beckmann, Svenja and Quack, Thomas and Grevelding, Christoph G. and Pinkerton, Anthony B. and Schönecker, Bruno and Burrows, Jeremy and Davioud-Charvet, Elisabeth and Rahlfs, Stefan and Becker, Katja. (2017) Arylmethylamino steroids as antiparasitic agents. Nature communications, 8. p. 14478.

Singh, Kawaljit and Okombo, John and Brunschwig, Christel and Ndubi, Ferdinand and Barnard, Linley and Wilkinson, Chad and Njogu, Peter M. and Njoroge, Mathew and Laing, Lizahn and Machado, Marta and Prudêncio, Miguel and Reader, Janette and Botha, Mariette and Nondaba, Sindisiwe and Birkholtz, Lyn-Marie and Lauterbach, Sonja and Churchyard, Alisje and Coetzer, Theresa L. and Burrows, Jeremy N. and Yeates, Clive and Denti, Paolo and Wiesner, Lubbe and Egan, Timothy J. and Wittlin, Sergio and Chibale, Kelly. (2017) Antimalarial pyrido[1,2-a]benzimidazoles : lead optimization, parasite life cycle stage profile, mechanistic evaluation, killing kinetics, and in vivo oral efficacy in a mouse model. Journal of medicinal chemistry, 60 (4). pp. 1432-1448.

Dong, Yuxiang and Wang, Xiaofang and Kamaraj, Sriraghavan and Bulbule, Vivek J. and Chiu, Francis C. K. and Chollet, Jacques and Dhanasekaran, Manickam and Hein, Christopher D. and Papastogiannidis, Petros and Morizzi, Julia and Shackleford, David M. and Barker, Helena and Ryan, Eileen and Scheurer, Christian and Tang, Yuanqing and Zhao, Qingjie and Zhou, Lin and White, Karen L. and Urwyler, Heinrich and Charman, William N. and Matile, Hugues and Wittlin, Sergio and Charman, Susan A. and Vennerstrom, Jonathan L.. (2017) Structure-activity relationship of the antimalarial ozonide artefenomel (OZ439). Journal of medicinal chemistry, 60 (7). pp. 2654-2668.

Leven, Michael and Knaab, Tanja C. and Held, Jana and Duffy, Sandra and Meister, Stephan and Fischli, Christoph and Meitzner, Diane and Lehmann, Ursula and Lungerich, Beate and Kuna, Krystina and Stahlke, Petra and Delves, Michael J. and Buchholz, Mirko and Winzeler, Elizabeth A. and Avery, Vicky M. and Mordmüller, Benjamin and Wittlin, Sergio and Kurz, Thomas. (2017) 3-hydroxy-N'-arylidenepropanehydrazonamides with halo-substituted phenanthrene scaffolds cure P. berghei infected mice when administered perorally. Journal of Medicinal Chemistry, 60 (14). pp. 6036-6044.

Abla, Nada and Bashyam, Sridevi and Charman, Susan A. and Greco, Béatrice and Hewitt, Philip and Jiménez-Díaz, Maria Belén and Katneni, Kasiram and Kubas, Holger and Picard, Didier and Sambandan, Yuvaraj and Sanz, Laura and Smith, Dennis and Wang, Tai and Willis, Paul and Wittlin, Sergio and Spangenberg, Thomas. (2017) Long-lasting and fast-acting in vivo efficacious antiplasmodial azepanylcarbazole amino alcohol. ACS medicinal chemistry letters, 8 (12). pp. 1304-1308.

Pavadai, E. and Kaur, G. and Wittlin, S. and Chibale, K.. (2017) Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. MedChemComm , 8 (6). pp. 1152-1157.

2016

Jourdan, Joëlle and Hugues, Matile and Reift, Ellen and Biehlmaier, Oliver and Dong, Yuxiang and Wang, Xiaofang and Mäser, Pascal and Vennerstrom, Jonathan and Wittlin, Sergio. (2016) Monoclonal antibodies that recognize the alkylation signature of antimalarial ozonides OZ277 (Arterolane) and OZ439 ( Artefenomel). ACS infectious diseases, 2 (1). pp. 54-61.

Pavadai, Elumalai and El Mazouni, Farah and Wittlin, Sergio and de Kock, Carmen and Phillips, Margaret A. and Chibale, Kelly. (2016) Identification of new human malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase inhibitors by pharmacophore and structure-based virtual screening. Journal of chemical information and modeling, 56 (3). pp. 548-562.

Le Bihan, Amélie and de Kanter, Ruben and Angulo-Barturen, Iñigo and Binkert, Christoph and Boss, Christoph and Brun, Reto and Brunner, Ralf and Buchmann, Stephan and Burrows, Jeremy and Dechering, Koen J. and Delves, Michael and Ewerling, Sonja and Ferrer, Santiago and Fischli, Christoph and Gamo-Benito, Francisco Javier and Gnädig, Nina F. and Heidmann, Bibia and Jiménez-Díaz, María Belén and Leroy, Didier and Martínez, Maria Santos and Meyer, Solange and Moehrle, Joerg J. and Ng, Caroline L. and Noviyanti, Rintis and Ruecker, Andrea and Sanz, Laura María and Sauerwein, Robert W. and Scheurer, Christian and Schleiferboeck, Sarah and Sinden, Robert and Snyder, Christopher and Straimer, Judith and Wirjanata, Grennady and Marfurt, Jutta and Price, Ric N. and Weller, Thomas and Fischli, Walter and Fidock, David A. and Clozel, Martine and Wittlin, Sergio. (2016) Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling. PLoS medicine, 13 (10). e1002138.

Norcross, Neil R. and Baragaña, Beatriz and Wilson, Caroline and Hallyburton, Irene and Osuna-Cabello, Maria and Norval, Suzanne and Riley, Jennifer and Stojanovski, Laste and Simeons, Frederick R. C. and Porzelle, Achim and Grimaldi, Raffaella and Wittlin, Sergio and Duffy, Sandra and Avery, Vicky M. and Meister, Stephan and Sanz, Laura and Jiménez-Díaz, Belén and Angulo-Barturen, Iñigo and Ferrer, Santiago and Martínez, María Santos and Gamo, Francisco Javier and Frearson, Julie A. and Gray, David W. and Fairlamb, Alan H. and Winzeler, Elizabeth A. and Waterson, David and Campbell, Simon F. and Willis, Paul and Read, Kevin D. and Gilbert, Ian H.. (2016) Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials. Journal of Medicinal Chemistry, 59 (13). pp. 6101-6120.

Ng, Caroline L. and Siciliano, Giulia and Lee, Marcus C. S. and de Almeida, Mariana J. and Corey, Victoria C. and Bopp, Selina E. and Bertuccini, Lucia and Wittlin, Sergio and Kasdin, Rachel G. and Le Bihan, Amélie and Clozel, Martine and Winzeler, Elizabeth A. and Alano, Pietro and Fidock, David A.. (2016) CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs. Molecular microbiology, 101 (3). pp. 381-393.

Boss, Christoph and Aissaoui, Hamed and Amaral, Nathalie and Bauer, Aude and Bazire, Stephanie and Binkert, Christoph and Brun, Reto and Bürki, Cédric and Ciana, Claire-Lise and Corminboeuf, Olivier and Delahaye, Stephane and Dollinger, Claire and Fischli, Christoph and Fischli, Walter and Flock, Alexandre and Frantz, Marie-Céline and Girault, Malory and Grisostomi, Corinna and Friedli, Astrid and Heidmann, Bibia and Hinder, Claire and Jacob, Gael and Le Bihan, Amelie and Malrieu, Sophie and Mamzed, Saskia and Merot, Aurelien and Meyer, Solange and Peixoto, Sabrina and Petit, Nolwenn and Siegrist, Romain and Trollux, Julien and Weller, Thomas and Wittlin, Sergio. (2016) Discovery and characterization of ACT-451840 : an antimalarial drug with a novel mechanism of action. ChemMedChem, 11 (18). pp. 1995-2014.

Williamson, Alice E. and Ylioja, Paul M. and Robertson, Murray N. and Antonova-Koch, Yevgeniya and Avery, Vicky and Baell, Jonathan B. and Batchu, Harikrishna and Batra, Sanjay and Burrows, Jeremy N. and Bhattacharyya, Soumya and Calderon, Felix and Charman, Susan A. and Clark, Julie and Crespo, Benigno and Dean, Matin and Debbert, Stefan L. and Delves, Michael and Dennis, Adelaide S. M. and Deroose, Frederik and Duffy, Sandra and Fletcher, Sabine and Giaever, Guri and Hallyburton, Irene and Gamo, Francisco-Javier and Gebbia, Marinella and Guy, R. Kiplin and Hungerford, Zoe and Kirk, Kiaran and Lafuente-Monasterio, Maria J. and Lee, Anna and Meister, Stephan and Nislow, Corey and Overington, John P. and Papadatos, George and Patiny, Luc and Pham, James and Ralph, Stuart A. and Ruecker, Andrea and Ryan, Eileen and Southan, Christopher and Srivastava, Kumkum and Swain, Chris and Tarnowski, Matthew J. and Thomson, Patrick and Turner, Peter and Wallace, Iain M. and Wells, Timothy N. C. and White, Karen and White, Laura and Willis, Paul and Winzeler, Elizabeth A. and Wittlin, Sergio and Todd, Matthew H.. (2016) Open source drug discovery : highly potent antimalarial compounds derived from the tres cantos arylpyrroles. ACS central science, 2 (10). pp. 687-701.

Baragaña, Beatriz and Norcross, Neil R. and Wilson, Caroline and Porzelle, Achim and Hallyburton, Irene and Grimaldi, Raffaella and Osuna-Cabello, Maria and Norval, Suzanne and Riley, Jennifer and Stojanovski, Laste and Simeons, Frederick R. C. and Wyatt, Paul G. and Delves, Michael J. and Meister, Stephan and Duffy, Sandra and Avery, Vicky M. and Winzeler, Elizabeth A. and Sinden, Robert E. and Wittlin, Sergio and Frearson, Julie A. and Gray, David W. and Fairlamb, Alan H. and Waterson, David and Campbell, Simon F. and Willis, Paul and Read, Kevin D. and Gilbert, Ian H.. (2016) Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy. Journal of medicinal chemistry, 59 (21). pp. 9672-9685.

Le Manach, Claire and Nchinda, Aloysius T. and Paquet, Tanya and Gonzàlez Cabrera, Diego and Younis, Yassir and Han, Ze and Bashyam, Sridevi and Zabiulla, Mohammed and Taylor, Dale and Lawrence, Nina and White, Karen L. and Charman, Susan A. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Botha, Mariëtte E. and Nondaba, Sindisiswe H. and Reader, Janette and Birkholtz, Lyn-Marie and Jiménez-Díaz, María Belén and Martínez, María Santos and Ferrer, Santiago and Angulo-Barturen, Iñigo and Meister, Stephan and Antonova-Koch, Yevgeniya and Winzeler, Elizabeth A. and Street, Leslie J. and Chibale, Kelly. (2016) Identification of a potential antimalarial drug candidate from a series of 2-aminopyrazines by optimization of aqueous solubility and potency across the parasite life cycle. Journal of medicinal chemistry, 59 (21). pp. 9890-9905.

2015

Chugh, Monika and Scheurer, Christian and Sax, Sibylle and Bilsland, Elizabeth and van Schalkwyk, Donelly A. and Wicht, Kathryn J. and Hofmann, Natalie and Sharma, Anil and Bashyam, Sridevi and Singh, Shivendra and Oliver, Stephen G. and Egan, Timothy J. and Malhotra, Pawan and Sutherland, Colin J. and Beck, Hans-Peter and Wittlin, Sergio and Spangenberg, Thomas and Ding, Xavier C.. (2015) Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains. Antimicrobial agents and chemotherapy, Vol. 59, H. 2. pp. 1110-1118.

Malmquist, Nicholas A. and Sundriyal, Sandeep and Caron, Joachim and Chen, Patty and Witkowski, Benoit and Menard, Didier and Suwanarusk, Rossarin and Renia, Laurent and Nosten, Francois and Jiménez-Díaz, María Belén and Angulo-Barturen, Iñigo and Martínez, María Santos and Ferrer, Santiago and Sanz, Laura M. and Gamo, Francisco-Javier and Wittlin, Sergio and Duffy, Sandra and Avery, Vicky M. and Ruecker, Andrea and Delves, Michael J. and Sinden, Robert E. and Fuchter, Matthew J. and Scherf, Artur. (2015) Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans. Antimicrobial agents and chemotherapy, Vol. 59, H. 2. pp. 950-959.

Brücher, Karin and Gräwert, Tobias and Konzuch, Sarah and Held, Jana and Lienau, Claudia and Behrendt, Christoph and Illarionov, Boris and Maes, Louis and Bacher, Adelbert and Wittlin, Sergio and Mordmüller, Benjamin and Fischer, Markus and Kurz, Thomas. (2015) Prodrugs of reverse fosmidomycin analogues. Journal of medicinal chemistry, 58 (4). pp. 2025-2035.

Witschel, Matthias C. and Rottmann, Matthias and Schwab, Anatol and Leartsakulpanich, Ubolsree and Chitnumsub, Penchit and Seet, Michael and Tonazzi, Sandro and Schwertz, Geoffrey and Stelzer, Frank and Mietzner, Thomas and McNamara, Case and Thater, Frank and Freymond, Céline and Jaruwat, Aritsara and Pinthong, Chatchadaporn and Riangrungroj, Pinpunya and Oufir, Mouhssin and Hamburger, Matthias and Mäser, Pascal and Sanz-Alonso, Laura M. and Charman, Susan and Wittlin, Sergio and Yuthavong, Yongyuth and Chaiyen, Pimchai and Diederich, François. (2015) Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT) : co-crystal structures of pyrazolopyrans with potent blood-and liver-stage activities. Journal of Medicinal Chemistry, 58 (7). pp. 3117-3130.

Baragaña, Beatriz and Hallyburton, Irene and Lee, Marcus C. S. and Norcross, Neil R. and Grimaldi, Raffaella and Otto, Thomas D. and Proto, William R. and Blagborough, Andrew M. and Meister, Stephan and Wirjanata, Grennady and Ruecker, Andrea and Upton, Leanna M. and Abraham, Tara S. and Almeida, Mariana J. and Pradhan, Anupam and Porzelle, Achim and Martínez, María Santos and Bolscher, Judith M. and Woodland, Andrew and Norval, Suzanne and Zuccotto, Fabio and Thomas, John and Simeons, Frederick and Stojanovski, Laste and Osuna-Cabello, Maria and Brock, Paddy M. and Churcher, Tom S. and Sala, Katarzyna A. and Zakutansky, Sara E. and Jiménez-Díaz, María Belén and Sanz, Laura Maria and Riley, Jennifer and Basak, Rajshekhar and Campbell, Michael and Avery, Vicky M. and Sauerwein, Robert W. and Dechering, Koen J. and Noviyanti, Rintis and Campo, Brice and Frearson, Julie A. and Angulo-Barturen, Iñigo and Ferrer-Bazaga, Santiago and Gamo, Francisco Javier and Wyatt, Paul G. and Leroy, Didier and Siegl, Peter and Delves, Michael J. and Kyle, Dennis E. and Wittlin, Sergio and Marfurt, Jutta and Price, Ric N. and Sinden, Robert E. and Winzeler, Elizabeth A. and Charman, Susan A. and Bebrevska, Lidiya and Gray, David W. and Campbell, Simon and Fairlamb, Alan H. and Willis, Paul A. and Rayner, Julian C. and Fidock, David A. and Read, Kevin D. and Gilbert, Ian H.. (2015) A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature, Vol. 522, H. 7556. pp. 315-320.

Phillips, Margaret A. and Lotharius, Julie and Marsh, Kennan and White, John and Dayan, Anthony and White, Karen L. and Njoroge, Jacqueline W. and El Mazouni, Farah and Lao, Yanbin and Kokkonda, Sreekanth and Tomchick, Diana R. and Deng, Xiaoyi and Laird, Trevor and Bhatia, Sangeeta N. and March, Sandra and Ng, Caroline L. and Fidock, David A. and Wittlin, Sergio and Lafuente-Monasterio, Maria and Benito, Francisco Javier Gamo and Alonso, Laura Maria Sanz and Martinez, Maria Santos and Jimenez-Diaz, Maria Belen and Bazaga, Santiago Ferrer and Angulo-Barturen, Iñigo and Haselden, John N. and Louttit, James and Cui, Yi and Sridhar, Arun and Zeeman, Anna-Marie and Kocken, Clemens and Sauerwein, Robert and Dechering, Koen and Avery, Vicky M. and Duffy, Sandra and Delves, Michael and Sinden, Robert and Ruecker, Andrea and Wickham, Kristina S. and Rochford, Rosemary and Gahagen, Janet and Iyer, Lalitha and Riccio, Ed and Mirsalis, Jon and Bathhurst, Ian and Rueckle, Thomas and Ding, Xavier and Campo, Brice and Leroy, Didier and Rogers, M. John and Rathod, Pradipsinh K. and Burrows, Jeremy N. and Charman, Susan A.. (2015) A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Science translational medicine, Vol. 7, H. 296 , 296ra111.

Gonzàlez Cabrera, Diego and Douelle, Frederic and Le Manach, Claire and Han, Ze and Paquet, Tanya and Taylor, Dale and Njoroge, Mathew and Lawrence, Nina and Wiesner, Lubbe and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Street, Leslie J. and Chibale, Kelly. (2015) Structure-activity relationship studies of orally active antimalarial 2,4-diamino-thienopyrimidines. Journal of medicinal chemistry, 58 (18). pp. 7572-7579.

Ongarora, Dennis S. B. and Strydom, Natasha and Wicht, Kathryn and Njoroge, Mathew and Wiesner, Lubbe and Egan, Timothy J. and Wittlin, Sergio and Jurva, Ulrik and Masimirembwa, Collen M. and Chibale, Kelly. (2015) Antimalarial benzoheterocyclic 4-aminoquinolines : structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. Bioorganic & medicinal chemistry, 23 (17). pp. 5419-5432.

Rusman, Yudi and Held, Benjamin W. and Blanchette, Robert A. and Wittlin, Sergio and Salomon, Christine E.. (2015) Soudanones A-G : antifungal isochromanones from the ascomycetous fungus Cadophora sp. isolated from an iron mine. Journal of natural products, Vol. 78, H. 6. pp. 1456-1460.

Kaur, G. and Singh, K. and Pavadai, E. and Njoroge, M. and Espinoza-Moraga, M. and de Kock, C. and Smith, P. J. and Wittlin, S. and Chibale, K.. (2015) Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G. MedChemComm, 6 (11). pp. 2023-2028.

Le Manach, Claire and Paquet, Tanya and Brunschwig, Christel and Njoroge, Mathew and Han, Ze and Gonzàlez Cabrera, Diego and Bashyam, Sridevi and Dhinakaran, Rajkumar and Taylor, Dale and Reader, Janette and Botha, Mariette and Churchyard, Alisje and Lauterbach, Sonja and Coetzer, Theresa L. and Birkholtz, Lyn-Marie and Meister, Stephan and Winzeler, Elizabeth A. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Jiménez-Díaz, María-Belén and Santos Martínez, María and Ferrer, Santiago and Angulo-Barturen, Iñigo and Street, Leslie J. and Chibale, Kelly. (2015) A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines. Journal of medicinal chemistry, 58 (21). pp. 8713-8722.

Wang, X. and Dong, Y. and Cal, M. and Kasier, M. and Wittling, S. and Vennerstrom, J. L.. (2015) Antiprotozoal selectivity of diimidazoline N-phenylbenzamides. ACS infectious diseases, 1. pp. 135-139.

Jortzik, Esther and Zocher, Kathleen and Isernhagen, Antje and Mailu, Boniface M. and Rahlfs, Stefan and Viola, Giampietro and Wittlin, Sergio and Hunt, Nicholas H. and Ihmels, Heiko and Becker, Katja. (2015) Benzo[b]quinolizinium derivatives have a strong antimalarial activity and inhibit indoleamine dioxygenase. Antimicrobial agents and chemotherapy, 60 (1). pp. 115-125.

2014

Le Manach, Claire and Gonzàlez Cabrera, Diego and Douelle, Frederic and Nchinda, Aloysius T. and Younis, Yassir and Taylor, Dale and Wiesner, Lubbe and White, Karen L. and Ryan, Eileen and March, Corinne and Duffy, Sandra and Avery, Vicky M. and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Charman, Susan A. and Street, Leslie J. and Chibale, Kelly. (2014) Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library : part 1. Journal of medicinal chemistry, 57 (6). pp. 2789-2798.

González Cabrera, Diego and Le Manach, Claire and Douelle, Frederic and Younis, Yassir and Feng, Tzu-Shean and Paquet, Tanya and Nchinda, Aloysius T. and Street, Leslie J. and Taylor, Dale and de Kock, Carmen and Wiesner, Lubbe and Duffy, Sandra and White, Karen L. and Zabiulla, K. Mohammed and Sambandan, Yuvaraj and Bashyam, Sridevi and Waterson, David and Witty, Michael J. and Charman, Susan A. and Avery, Vicky M. and Wittlin, Sergio and Chibale, Kelly. (2014) 2,4-diaminothienopyrimidines as orally active antimalarial agents. Journal of medicinal chemistry, 57 (3). pp. 1014-1022.

Mizukawa, Yuki and Ge, Jian-Feng and Bakar Md, Abu and Itoh, Isamu and Scheurer, Christian and Wittlin, Sergio and Brun, Reto and Matsuoka, Hiroyuki and Ihara, Masataka. (2014) Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites. Bioorganic & medicinal chemistry, 22 (14). pp. 3749-3752.

Leven, Michael and Held, Jana and Duffy, Sandra and Tschan, Serena and Sax, Sibylle and Kamber, Jolanda and Frank, Walter and Kuna, Krystina and Geffken, Detlef and Siethoff, Christoph and Barth, Stéphane and Avery, Vicky M. and Wittlin, Sergio and Mordmüller, Benjamin and Kurz, Thomas. (2014) Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides. Journal of medicinal chemistry, 57 (19). pp. 7971-7976.

Le Manach, Claire and Paquet, Tanya and Gonzàlez Cabrera, Diego and Younis, Yassir and Taylor, Dale and Wiesner, Lubbe and Lawrence, Nina and Schwager, Sylva and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Street, Leslie J. and Chibale, Kelly. (2014) Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library : part 2. Journal of medicinal chemistry, 57 (21). pp. 8839-8848.

2013

Abiodun, Oyindamola O. and Brun, Reto and Wittlin, Sergio. (2013) In vitro interaction of artemisinin derivatives or the fully synthetic peroxidic anti-malarial OZ277 with thapsigargin in Plasmodium falciparum strains. Malaria journal, Vol. 12 , 43.

Moehrle, J. J. and Duparc, S. and Siethoff, C. and van Giersbergen, P. L. and Craft, J. C. and Arbe-Barnes, S. and Charman, S. A. and Gutierrez, M. and Wittlin, S. and Vennerstrom, J. L.. (2013) First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials. British journal of clinical pharmacology, Vol. 75, H. 2. pp. 535-548.

Wang, X. and Dong, Y. and Wittlin, S. and Charman, S. A. and Chiu, F. C. and Chollet, J. and Katneni, K. and Mannila, J. and Morizzi, J. and Ryan, E. and Scheurer, C. and Steuten, J. and Santo, Tomas J. and Snyder, C. and Vennerstrom, J. L.. (2013) Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. Journal of medicinal chemistry, 56 (6). pp. 2547-2555.

Ciana, C. L. and Siegrist, R. and Aissaoui, H. and Marx, L. and Racine, S. and Meyer, S. and Binkert, C. and de Kanter, R. and Fischli, C. and Wittlin, S. and Boss, C.. (2013) Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 23, H. 3. pp. 658-662.

Hao, Hong-Dong and Wittlin, Sergio and Wu, Yikang. (2013) Potent antimalarial 1,2,4-trioxanes through perhydrolysis of epoxides. Chemistry : a European journal, Vol. 19, H. 23. pp. 7605-7619.

Nsumiwa, Samkele and Kuter, David and Wittlin, Sergio and Chibale, Kelly and Egan, Timothy J.. (2013) Structure-activity relationships for ferriprotoporphyrin IX association and β-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods. Bioorganic & medicinal chemistry, 21 (13). pp. 3738-3748.

Le Manach, Claire and Scheurer, Christian and Sax, Sibylle and Schleiferböck, Sarah and Gonzalez Cabrera, Diego and Younis, Yassir and Paquet, Tanya and Street, Leslie and Smith, Peter and Ding, Xavier and Waterson, David and Witty, Michael J. and Leroy, Didier and Chibale, Kelly and Wittlin, Sergio. (2013) Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum. Malaria journal, Vol. 12 , 424.

Brunner, R. and Ng, C. L. and Aissaoui, H. and Akabas, M. H. and Boss, C. and Brun, R. and Callaghan, P. S. and Corminboeuf, O. and Fidock, D. A. and Frame, I. J. and Heidmann, B. and Le Bihan, A. and Jeno, P. and Mattheis, C. and Moes, S. and Muller, I. B. and Paguio, M. and Roepe, P. D. and Siegrist, R. and Voss, Till S. and Welford, R. W. and Wittlin, S. and Binkert, C.. (2013) UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells. Journal of biological chemistry, Vol. 288, H. 31. pp. 22576-22583.

Younis, Yassir and Douelle, Frederic and González Cabrera, Diego and Le Manach, Claire and Nchinda, Aloysius T. and Paquet, Tanya and Street, Leslie J. and White, Karen L. and Zabiulla, K. Mohammed and Joseph, Jayan T. and Bashyam, Sridevi and Waterson, David and Witty, Michael J. and Wittlin, Sergio and Charman, Susan A. and Chibale, Kelly. (2013) Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity. Journal of medicinal chemistry, 56 (21). pp. 8860-8871.

Schleiferböck, Sarah and Scheurer, Christian and Ihara, Masataka and Itoh, Isamu and Bathurst, Ian and Burrows, Jeremy N. and Fantauzzi, Pascal and Lotharius, Julie and Charman, Susan A. and Morizzi, Julia and Shackleford, David M. and White, Karen L. and Brun, Reto and Wittlin, Sergio. (2013) In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models. Drug design, development and therapy, Vol. 7. pp. 1377-1384.

2012

Wenzler, T. and Steinhuber, A. and Wittlin, S. and Scheurer, C. and Brun, R. and Trampuz, A.. (2012) Isothermal microcalorimetry, a new tool to monitor drug action against Trypanosoma brucei and Plasmodium falciparum. PLoS neglected tropical diseases, Vol. 6, H. 6 , e1668.

Mäser, P. and Wittlin, S. and Rottmann, M. and Wenzler, T. and Kaiser, M. and Brun, R.. (2012) Antiparasitic agents : new drugs on the horizon. Current opinion in pharmacology, Vol. 12, H. 5. pp. 562-566.

Brunner, R. and Aissaoui, H. and Boss, C. and Bozdech, Z. and Brun, R. and Corminboeuf, O. and Delahaye, S. and Fischli, C. and Heidmann, B. and Kaiser, M. and Kamber, J. and Meyer, S. and Papastogiannidis, P. and Siegrist, R. and Voss, Till S. and Welford, R. and Wittlin, S. and Binkert, C.. (2012) Identification of a new chemical class of antimalarials. Journal of infectious diseases, Vol. 206, no. 5. pp. 735-743.

Dreyer, A. M. and Matile, H. and Papastogiannidis, P. and Kamber, J. and Favuzza, P. and Voss, Till S. and Wittlin, S. and Pluschke, G.. (2012) Passive immunoprotection of Plasmodium falciparum-infected mice designates the CyRPA as candidate malaria vaccine antigen. Journal of immunology : official journal of the American Association of Immunologists, Vol. 188, H. 12. pp. 6225-6237.

Edlin, C. D. and Morgans, G. and Winks, S. and Duffy, S. and Avery, V. M. and Wittlin, S. and Waterson, D. and Burrows, J. and Bryans, J.. (2012) Identification and in-vitro ADME assessment of a series of novel anti-malarial agents suitable for hit-to-lead chemistry. ACS medicinal chemistry letters, Vol. 3, H. 7. pp. 570-573.

Li, Y. and Hao, H. D. and Wittlin, S. and Wu, Y.. (2012) Simple analogues of Qinghaosu (Artemisinin). Chemistry : an Asian journal / an ACES journal, Vol. 7, H. 8. pp. 1881-1886.

Delves, M. and Plouffe, D. and Scheurer, C. and Meister, S. and Wittlin, S. and Winzeler, E. A. and Sinden, R. E. and Leroy, D.. (2012) The activities of current antimalarial drugs on the life cycle stages of Plasmodium : a comparative study with human and rodent parasites. PLoS medicine, Vol. 9, H. 2 , e1001169.

González, Cabrera and Douelle, F. and Younis, Y. E. and Feng, T. S. and Lemanach, C. and Nchinda, A. T. and Street, L. J. and Scheurer, C. and Kamber, J. and White, K. L. and Montagnat, O. D. and Ryan, E. and Katneni, K. and Zabiulla, K. M. and Joseph, J. T. and Bashyam, S. and Waterson, D. and Witty, M. J. and Charman, S. A. and Wittlin, S. and Chibale, K.. (2012) Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. Journal of medicinal chemistry, 55 (24). pp. 11022-11030.

Younis, Y. and Douelle, F. and Feng, T. S. and Cabrera, D. G. and Manach, C. L. and Nchinda, A. T. and Duffy, S. and White, K. L. and Shackleford, D. M. and Morizzi, J. and Mannila, J. and Katneni, K. and Bhamidipati, R. and Zabiulla, K. M. and Joseph, J. T. and Bashyam, S. and Waterson, D. and Witty, M. J. and Hardick, D. and Wittlin, S. and Avery, V. and Charman, S. A. and Chibale, K.. (2012) 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. Journal of medicinal chemistry, 55 (7). pp. 3479-3487.

Marfurt, J. and Chalfein, F. and Prayoga, P. and Wabiser, F. and Wirjanata, G. and Sebayang, B. and Piera, K. A. and Wittlin, S. and Haynes, R. K. and Mohrle, J. J. and Anstey, N. M. and Kenangalem, E. and Price, R. N.. (2012) Comparative ex vivo activity of novel endoperoxides in multidrug-resistant Plasmodium falciparum and P. vivax. Antimicrobial agents and chemotherapy : AAC, Vol. 56, H. 10. pp. 5258-5263.

Li, Y. and Wittlin, S. and Wu, Y.. (2012) Access to some UV chromophore-containing antimalarial trioxanes using hydrogen peroxide as source of the peroxy bonds. Heterocycles : an international journal for reviews and communications in heterocyclic chemistry, Vol. 84, H. 2. pp. 1217-1226.

Wittlin, S. and Ekland, E. and Craft, J. C. and Lotharius, J. and Bathurst, I. and Fidock, D. A. and Fernandes, P.. (2012) In vitro and in vivo activity of Solithromycin (CEM-101) against Plasmodium species. Antimicrobial agents and chemotherapy : AAC, Vol. 56, H. 2. pp. 703-707.

2011

Chadwick, J. and Amewu, R. K. and Marti, F. and Bousejra-El Garah F., and Sharma, R. and Berry, N. G. and Stocks, P. A. and Burrell-Saward H., and Wittlin, S. and Rottmann, M. and Brun, R. and Taramelli, D. and Parapini, S. and Ward, S. A. and O'Neill P. M., . (2011) Antimalarial mannoxanes : hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action. ChemMedChem : chemistry enabling drug discovery, Vol. 6, H. 8. pp. 1357-1361.

Shi, X. L. and Ge, J. F. and Liu, B. Q. and Kaiser, M. and Wittlin, S. and Brun, R. and Ihara, M.. (2011) Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 21, H. 19. pp. 5804-5807.

Lu, Y. T. and Arai, C. and Ge, J. F. and Ren, W. S. and Kaiser, M. and Wittlin, S. and Brun, R. and Lu, J. M. and Ihara, M.. (2011) Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive phenothiazinium chlorides. Dyes and pigments : an international journal, Vol. 89, H. 1. pp. 44-48.

Charman, S. A. and Arbe-Barnes S., and Bathurst, I. C. and Brun, R. and Campbell, M. and Charman, W. N. and Chiu, F. C. and Chollet, J. and Craft, J. C. and Creek, D. J. and Dong, Y. and Matile, H. and Maurer, M. and Morizzi, J. and Nguyen, T. and Papastogiannidis, P. and Scheurer, C. and Shackleford, D. M. and Sriraghavan, K. and Stingelin, L. and Tang, Y. and Urwyler, H. and Wang, X. and White, K. L. and Wittlin, S. and Zhou, L. and Vennerstrom, J. L.. (2011) Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria. Proceedings of the National Academy of Sciences of the United States of America, Vol. 108, H. 11. pp. 4400-4405.

Schiaffo, C. E. and Rottmann, M. and Wittlin, S. and Dussault, P. H.. (2011) 3-alkoxy-1,2-dioxolanes : synthesis and evaluation as potential antimalarial agents. ACS medicinal chemistry letters, Vol. 2, H. 4. pp. 316-319.

Skerlj, R. T. and Bastos, C. M. and Booker, M. L. and Kramer, M. L. and Barker, R. H. and Celatka, C. A. and O'Shea T. J., and Munoz, B. and Sidhu, A. B. and Cortese, J. F. and Wittlin, S. and Papastogiannidis, P. and Angulo-Barturen I., and Jimenez-Diaz M. B., and Sybertz, E.. (2011) Optimization of potent inhibitors of P. falciparum dihydroorotate dehydrogenase for the treatment of malaria. ACS medicinal chemistry letters, Vol. 2, H. 9. pp. 708-713.

González Cabrera D., and Douelle, F. and Feng, T. S. and Nchinda, A. T. and Younis, Y. and White, K. L. and Wu, Q. and Ryan, E. and Burrows, J. N. and Waterson, D. and Witty, M. J. and Wittlin, S. and Charman, S. A. and Chibale, K.. (2011) Novel orally active antimalarial thiazoles. Journal of medicinal chemistry, 54 (21). pp. 7713-7719.

Vargas, S. and Ndjoko Ioset K., and Hay, A. E. and Ioset, J. R. and Wittlin, S. and Hostettmann, K.. (2011) Screening medicinal plants for the detection of novel antimalarial products applying the inhibition of beta-hematin formation. Journal of pharmaceutical and biomedical analysis, Vol. 56, H. 5. pp. 880-886.

Baschong, Werner and Wittlin, Sergio and Inglis, Kirstine A. and Fairlamb, Alan H. and Croft, Simon L. and Kumar, T. R. Santha and Fidock, David A. and Brun, Reto. (2011) Triclosan is minimally effective in rodent malaria models. Nature medicine, Vol. 17. pp. 33-34.

Barker, R. H. Jr. and Urgaonkar, S. and Mazitschek, R. and Celatka, C. and Skerlj, R. and Cortese, J. F. and Tyndall, E. and Liu, H. and Cromwell, M. and Sidhu, A. B. and Guerrero-Bravo, J. E. and Crespo-Llado, K. N. and Serrano, A. E. and Lin, J. W. and Janse, C. J. and Khan, S. M. and Duraisingh, M. and Coleman, B. I. and Angulo-Barturen, I. and Jimenez-Diaz, M. B. and Magan, N. and Gomez, V. and Ferrer, S. and Martinez, M. S. and Wittlin, S. and Papastogiannidis, P. and O'Shea, T. and Klinger, J. D. and Bree, M. and Lee, E. and Levine, M. and Wiegand, R. C. and Munoz, B. and Wirth, D. F. and Clardy, J. and Bathurst, I. and Sybertz, E.. (2011) Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum. Antimicrobial agents and chemotherapy, 55 (6). pp. 2612-2622.

2010

Booker, M. L. and Bastos, C. M. and Kramer, M. L. and Barker, R. H. and Skerlj, R. and Sidhu, A. B. and Deng, X. and Celatka, C. and Cortese, J. F. and Guerrero Bravo J. E., and Crespo Llado K. N., and Serrano, A. E. and Angulo-Barturen I., and Jimenez-Diaz M. B., and Viera, S. and Garuti, H. and Wittlin, S. and Papastogiannidis, P. and Lin, J. W. and Janse, C. J. and Khan, S. M. and Duraisingh, M. and Coleman, B. and Goldsmith, E. J. and Phillips, M. A. and Munoz, B. and Wirth, D. F. and Klinger, J. D. and Wiegand, R. and Sybertz, E.. (2010) Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model. Journal of Biological Chemistry, Vol. 285, H. 43. pp. 33054-33064.

Tang, Y. and Wittlin, S. and Charman, S. A. and Chollet, J. and Chiu, F. C. and Morizzi, J. and Johnson, L. M. and Tomas, J. S. and Scheurer, C. and Snyder, C. and Zhou, L. and Dong, Y. and Charman, W. N. and Matile, H. and Urwyler, H. and Dorn, A. and Vennerstrom, J. L.. (2010) The comparative antimalarial properties of weak base and neutral synthetic ozonides. Bioorganic and Medicinal Chemistry Letters, Vol. 20, H. 2. pp. 563-566.

Dong, Y. and McCullough, K. J. and Wittlin, S. and Chollet, J. and Vennerstrom, J. L.. (2010) The structure and antimalarial activity of dispiro-1,2,4,5-tetraoxanes derived from (+)-dihydrocarvone. Bioorganic and Medicinal Chemistry Letters, Vol. 20, H. 22. pp. 6359-6361.

O'Neill P. M., and Amewu, R. K. and Nixon, G. L. and Bousejra, E. F. and Mungthin, M. and Chadwick, J. and Shone, A. E. and Vivas, L. and Lander, H. and Barton, V. and Muangnoicharoen, S. and Bray, P. G. and Davies, J. and Park, B. K. and Wittlin, S. and Brun, R. and Preschel, M. and Zhang, K. and Ward, S. A.. (2010) Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins. Angewandte Chemie. International edition in English, Vol. 49, H. 33. pp. 5693-5697.

Wright, C. W. and Linley, P. A. and Brun, R. and Wittlin, S. and Hsu, E.. (2010) Ancient Chinese methods are remarkably effective for the preparation of artemisinin-rich extracts of Qing Hao with potent antimalarial activity. Molecules, Vol. 15, H. 2. pp. 804-812.

Dong, Y. and Wittlin, S. and Sriraghavan, K. and Chollet, J. and Charman, S. A. and Charman, W. N. and Scheurer, C. and Urwyler, H. and Santo, T. J. and Snyder, C. and Creek, D. J. and Morizzi, J. and Koltun, M. and Matile, H. and Wang, X. and Padmanilayam, M. and Tang, Y. and Dorn, A. and Brun, R. and Vennerstrom, J. L.. (2010) The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). Journal of Medicinal Chemistry, 53 (1). pp. 481-491.

Nzila, A. and Rottmann, M. and Chitnumsub, P. and Kiara, S. M. and Kamchonwongpaisan, S. and Maneeruttanarungroj, C. and Taweechai, S. and Yeung, B. K. and Goh, A. and Lakshminarayana, S. B. and Zou, B. and Wong, J. and Ma, N. L. and Weaver, M. and Keller, T. H. and Dartois, V. and Wittlin, S. and Brun, R. and Yuthavong, Y. and Diagana, T. T.. (2010) Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. Antimicrobial agents and chemotherapy : AAC, Vol. 54, H. 6. pp. 2603-2610.

Burgess, S. J. and Kelly, J. X. and Shomloo, S. and Wittlin, S. and Brun, R. and Liebmann, K. and Peyton, D. H.. (2010) Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. Journal of medicinal chemistry, 53 (17). pp. 6477-6489.

Abiodun, O. O. and Gbotosho, G. O. and Ajaiyeoba, E. O. and Happi, C. T. and Hofer, S. and Wittlin, S. and Sowunmi, A. and Brun, R. and Oduola, A. M. J.. (2010) Comparison of SYBR Green I-, PicoGreen-, and [H-3]-hypoxanthine-based assays for in vitro antimalarial screening of plants from Nigerian ethnomedicine. Parasitology research : Organ der Deutschen Gesellschaft für Parasitologie, Vol. 106, H. 4. pp. 933-939.

Ge, J. F. and Arai, C. and Yang, M. and Bakar, M. A. and Lu, J. and Ismail, N. S. M. and Wittlin, S. and Kaiser, M. and Brun, R. and Charman, S. A. and Nguyen, T. and Morizzi, J. and Itoh, I. and Ihara, M.. (2010) Discovery of novel benzo[a]phenoxazine SSJ-183 as a drug candidate for malaria. ACS medicinal chemistry letters, Vol. 1, H. 7. pp. 360-364.

2009

Tritten, L. and Matile, H. and Brun, R. and Wittlin, S.. (2009) A new double-antibody sandwich ELISA targeting Plasmodium falciparum aldolase to evaluate anti-malarial drug sensitivity. Malaria Journal, Vol. 8 , 226.

Kelly, J. X. and Smilkstein, M. J. and Brun, R. and Wittlin, S. and Cooper, R. A. and Lane, K. D. and Janowsky, A. and Johnson, R. A. and Dodean, R. A. and Winter, R. and Hinrichs, D. J. and Riscoe, M. K.. (2009) Discovery of dual function acridones as a new antimalarial chemotype. Nature, Vol. 459, H. 7244. pp. 270-273.

Kiboi, D. M. and Irungu, B. N. and Langat, B. and Wittlin, S. and Brun, R. and Chollet, J. and Abiodun, O. and Nganga, J. K. and Nyambati, V. C. and Rukunga, G. M. and Bell, A. and Nzila, A.. (2009) Plasmodium berghei ANKA: selection of resistance to piperaquine and lumefantrine in a mouse model. Experimental parasitology : EP, Vol. 122, H. 3. pp. 196-202.

Pudhom, K. and Ge, M. F. and Arai, C. and Yang, M. and Kaiser, M. and Wittlin, S. and Brun, R. and Itoh, I. and Ihara, M.. (2009) Synthesis and biological properties of a rhodacyanine derivative, Ssj-127, having high efficacy against malaria protozoa. Heterocycles : an international journal for reviews and communications in heterocyclic chemistry, Vol. 77, H. 1. pp. 207-210.

Efange, S. M. and Brun, R. and Wittlin, S. and Connolly, J. D. and Hoye, T. R. and McAkam, T. and Makolo, F. L. and Mbah, J. A. and Nelson, D. P. and Nyongbela, K. D. and Wirmum, C. K.. (2009) Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity. Journal of Natural Products, Vol. 72, H. 2. pp. 280-283.

Sturm, N. and Hu, Y. and Zimmermann, H. and Fritz-Wolf K., and Wittlin, S. and Rahlfs, S. and Becker, K.. (2009) Compounds structurally related to ellagic acid show improved antiplasmodial activity. Antimicrobial agents and chemotherapy : AAC, Vol. 53, H. 2. pp. 622-630.

Irungu, B. and Kiboi, D. and Langat, B. and Rukunga, G. and Wittlin, S. and Nzila, A.. (2009) Methotrexate and aminopterin lack in vivo antimalarial activity against murine malaria species. Experimental parasitology : EP, Vol. 123, H. 2. pp. 118-121.

Wang, X. and Creek, D. J. and Schiaffo, C. E. and Dong, Y. and Chollet, J. and Scheurer, C. and Wittlin, S. and Charman, S. A. and Dussault, P. H. and Wood, J. K. and Vennerstrom, J. L.. (2009) Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs : relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity. Bioorganic & medicinal chemistry letters : a Tetrahedron publication for the rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Vol. 19, H. 16. pp. 4542-4545.

Nyongbela, Kennedy and Ndjoko, Karine Ioset and Brun, Reto and Wittlin, Sergio and Mbah, James and Makolo, Felix and Akam, Marc and Wirmum, Claire and Efange, Simon and Hostettmann, Kurt. (2009) Occurrence of sesquiterpene derivatives in Scleria striatonux de wild (Cyperaceae). Natural product communications : NPC, Vol. 4, H. 1. pp. 5-8.