Rational modification of a candidate cancer drug for use against Chagas disease

…, CLMJ Verlinde, M Karimi, GI Lepesheva…

Index: Kraus, James M.; Verlinde, Christophe L. M. J.; Karimi, Mandana; Lepesheva, Galina I.; Gelb, Michael H.; Buckner, Frederick S. Journal of Medicinal Chemistry, 2009 , vol. 52, # 6 p. 1639 - 1647

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Citation Number: 99

Abstract

Chagas disease is one of the major neglected diseases of the world. Existing drug therapies are limited, ineffective, and highly toxic. We describe a novel strategy of drug discovery of adapting an existing clinical compound with excellent pharmaceutical properties to target a pathogenic organism. The protein farnesyltransferase (PFT) inhibitor tipifarnib, now in phase III anticancer clinical trials, was previously found to kill Trypanosoma cruzi by blocking ...