Items where Author is "Beaufils, Florent"

2020

Borsari, Chiara and Keles, Erhan and Rageot, Denise and Treyer, Andrea and Bohnacker, Thomas and Bissegger, Lukas and De Pascale, Martina and Melone, Anna and Sriramaratnam, Rohitha and Beaufils, Florent and Hamburger, Matthias and Hebeisen, Paul and Löscher, Wolfgang and Fabbro, Doriano and Hillmann, Petra and Wymann, Matthias P.. (2020) 4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of neurological disorders. Journal of Medicinal Chemistry, 63 (22). pp. 13595-13617.

2017

Beaufils, Florent and Cmiljanovic, Natasa and Cmiljanovic, Vladimir and Bohnacker, Thomas and Melone, Anna and Marone, Romina and Jackson, Eileen and Zhang, Xuxiao and Sele, Alexander and Borsari, Chiara and Mestan, Jurgen and Hebeisen, Paul and Hillmann, Petra and Giese, Bernd and Zvelebil, Marketa and Fabbro, Doriano and Williams, Roger L. and Rageot, Denise and Wymann, Matthias P.. (2017) 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. Journal of Medicinal Chemistry, 60 (17). pp. 7524-7538.

Bohnacker, Thomas and Prota, Andrea E. and Beaufils, Florent and Burke, John E. and Melone, Anna and Inglis, Alison J. and Rageot, Denise and Sele, Alexander M. and Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Bargsten, Katja and Aher, Amol and Akhmanova, Anna and Fernando Diaz, J. and Fabbro, Doriano and Zvelebil, Marketa and Williams, Roger L. and Steinmetz, Michel O. and Wymann, Matthias P.. (2017) Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention. Nature communications, 8. p. 14683.

2016

Sele, Alexander M. and Rageot, Denise and Bohnacker, Thomas and Beaufils, Florent and Prota, Andrea E. and Steinmetz, Michel O. and Wymann, Matthias P.. (2016) Novel 4-(pyrimidin-2-yl)morpholines targeting the colchicine-binding site of tubulin. Cancer Research, 76 (14). p. 1364.

Beaufils, Florent and Rageot, Denise and Melone, Anna and Sele, Alexander and Lang, Marc and Mestan, Juergen and Ettlin, Robert A. and Hillmann, Petra and Cmiljanovic, Vladimir and Walter, Carolin and Singer, Elisabeth and Nguyen, Hoa H. P. and Hebeisen, Paul and Fabbro, Dorian and Wymann, Matthias P.. (2016) Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620. Cancer Research, 76 (14). 393A.

Beaufils, Florent and Rageot, Denise and Melone, Anna and Lang, Marc and Mestan, Jürgen and Cmiljanovic, Vladimir and Hillmann, Petra and Hebeisen, Paul and Fabbro, Doriano and Wymann, Matthias P.. (2016) Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor. Cancer Research, 76 (14). p. 1336.

2015

Bohnacker, Thomas and Beaufils, Florent and Prota, Andrea E. and Burke, John E. and Melone, Anna and Inglis, Alison J. and Fusco, Ludovico and Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Rageot, Denise and Bargsten, Katja and Saez-Calvo, Gonzalo and Pertz, Olivier and Aher, Amol B. and Akhmanova, Anna and Diaz, Fernando J. and Fabbro, Doriano and Zvelebil, Marketa and Williams, Roger L. and Steinmetz, Michel O. and Wymann, Matthias P.. (2015) BKM120-mediated G2 arrest: Structural and functional segregation of off-target action and PI3K inhibition. Cancer Research, 75 (15). p. 671.

Cmiljanovic, Vladimir and Cmiljanovic, Natasa and Marone, Romina and Beaufils, Florent and Zhang, Xuxiao and Zvelebil, Marketa and Hebeisen, Paul and Lang, Marc and Mestan, Juergen and Melone, Anna and Bohnacker, Thomas and Gaudio, Eugenio and Tarantelli, Chiara and Bertoni, Francesco and Ritschard, Reto and Pretre, Vincent and Wicki, Andreas and Fabbro, Doriano and Hillmann, Petra and Williams, Roger and Giese, Bernd and Wymann, Matthias P.. (2015) PQR309: Structure-based design, synthesis and biological evaluation of a novel, selective, dual pan-PI3K/mTOR inhibitor. Cancer Research, 75 (15). p. 2664.

Tarantelli, Chiara and Gaudio, Eugenio and Kwee, Ivo and Rinaldi, Andrea and Bernasconi, Elena and Cascione, Luciano and Hillmann, Petra and Stathis, Anastasios and Carrassa, Laura and Broggini, Massimo and Stussi, Georg and Fabbro, Doriano and Beaufils, Florent and Melone, Anna and Bohnacker, Thomas and Wymann, Matthias P. and Wicki, Andreas and Zucca, Emanuele and Cmiljanovic, Vladimir and Bertoni, Francesco. (2015) Pre-clinical activity and mechanism of action of the novel dual PI3K/mTOR inhibitor PQR309 in B-cell lymphomas. Cancer Research, 75 (15). p. 2652.

2014

Zimmermann, Mirjam and Cal, Ruben and Janett, Elia and Hoffmann, Viktor and Bochet, Christian G. and Constable, Edwin and Beaufils, Florent and Wymann, Matthias P.. (2014) Cell-Permeant and Photocleavable Chemical Inducer of Dimerization. Angewandte Chemie International Edition, 53 (18). pp. 4717-4720.