Synthesis and antimalarial evaluation of novel isocryptolepine derivatives

LR Whittell, KT Batty, RPM Wong, EM Bolitho…

Index: Whittell, Louise R.; Batty, Kevin T.; Wong, Rina P.M.; Bolitho, Erin M.; Fox, Simon A.; Davis, Timothy M.E.; Murray, Paul E. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 24 p. 7519 - 7525

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Citation Number: 27

Abstract

A series of mono-and di-substituted analogues of isocryptolepine have been synthesized and evaluated for in vitro antimalarial activity against chloroquine sensitive (3D7) and resistant (W2mef) Plasmodium falciparum and for cytotoxicity (3T3 cells). Di-halogenated compounds were the most potent derivatives and 8-bromo-2-chloroisocryptolepine displayed the highest selectivity index (106; the ratio of cytotoxicity (IC50= 9005nM) to ...