Novel nucleoside-based antimalarial compounds

Zheng, Zhaoyan and Tran, Huu-Anh and Manivannan, Srinivasan and Wen, Xianghui and Kaiser, Marcel and Brun, Reto and Snyder, Floyd F. and Back, Thomas G.. (2016) Novel nucleoside-based antimalarial compounds. Bioorganic & medicinal chemistry letters, 26 (12). pp. 2861-2865.

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Official URL: http://edoc.unibas.ch/43680/

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The malaria-causing parasite Plasmodium falciparum employs a salvage pathway for the biosynthesis of nucleotides, in contrast to de novo biosynthesis that is utilized by the human host. A series of twenty-two 2-, 6- and 5'-modified adenosine ribonucleosides was synthesized, with the expectation that these compounds would generate toxic metabolites instead of active nucleotides by the pathogen, while remaining inert in host cells. Bioassays with P. falciparum (K1 strain) indicated IC50 values as low as 110nM and a selectivity index with respect to cytotoxicity toward an L6 rat myoblast cell line of >1000 for the most potent analogue.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:30 Aug 2016 09:17
Deposited On:30 Aug 2016 09:17

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