Synthesis and antimalarial evaluation of novel isocryptolepine derivatives

L.R. Whittell, K.T. Batty, R.P.M. Wong, E.M. Bolitho, Simon Fox, Timothy Davis, P.E. Murray

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    56 Citations (Scopus)

    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. © 2011 Elsevier Ltd. All rights reserved.
    Original languageEnglish
    Pages (from-to)7519-7525
    JournalBioorganic and Medicinal Chemistry
    Volume19
    Issue number24
    DOIs
    Publication statusPublished - 2011

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