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ABSTRACT:
SUBMITTER: Kraus JM
PROVIDER: S-EPMC2877169 | biostudies-literature | 2010 May
REPOSITORIES: biostudies-literature
Kraus James M JM Tatipaka Hari Babu HB McGuffin Sarah A SA Chennamaneni Naveen Kumar NK Karimi Mandana M Arif Jenifer J Verlinde Christophe L M J CL Buckner Frederick S FS Gelb Michael H MH
Journal of medicinal chemistry 20100501 10
We previously reported that the cancer drug clinical candidate tipifarnib kills the causative agent of Chagas disease, Trypanosoma cruzi, by blocking ergosterol biosynthesis at the level of inhibition of lanosterol 14alpha-demethylase. Tipifarnib is an inhibitor of human protein farnesyltransferase. We synthesized tipifarnib analogues that no longer bind to protein farnesyltransferase and display increased potency for killing parasites. This was achieved in a structure-guided fashion by changing ...[more]