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  • Title: Synthesis and antimalarial evaluation of novel isocryptolepine derivatives.
    Author: Whittell LR, Batty KT, Wong RP, Bolitho EM, Fox SA, Davis TM, Murray PE.
    Journal: Bioorg Med Chem; 2011 Dec 15; 19(24):7519-25. PubMed ID: 22055713.
    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 (IC(50)=9005 nM) to antimalarial activity (IC(50)=85 nM)). Our evaluation of novel isocryptolepine compounds has demonstrated that di-halogenated derivatives are promising antimalarial lead compounds.
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