Synthesis and antimalarial evaluation of novel isocryptolepine derivatives

Louise R Whittell, Kevin T Batty, Rina P M Wong, Erin M Bolitho, Simon A Fox, Timothy M E Davis, Paul E Murray

Research output: Contribution to journalArticlepeer-review

57 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)7519-25
Number of pages7
JournalBioorganic & Medicinal Chemistry
Issue number24
Publication statusPublished - 2011


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