Kumar, R and D, Mohanakrishnan and Sharma , A and Kaushik, N K and Kalia, K and Sinha, Arun K and Sahal, D (2010) Reinvestigation of structure–activity relationship of methoxylated chalcones as antimalarials: Synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone. European Journal of Medicinal Chemistry, 45. pp. 5292-5301.

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We have examined the antimalarial structure–activity relationship of a series of methoxylated chalcones (A–CH CH–CO–B) against Plasmodium falciparum (3D7 strain) using fluorescence-based SYBR Green assay. Our study has revealed that electron releasing methoxy groups on ring A and electron withdrawing groups on ring B increases antimalarial potency while the positional interchange of these groups causes a decrease. In particular, 2,4,5-trimethoxy substitution pattern at ring A provided potent analogues which were easily derived from abundantly available natural β-asarone rich Acorus calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC50: 1.8 μM) and 26 (IC50: 2 μM) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum.

Item Type: Article
Uncontrolled Keywords: Chalcones; Antimalarial; Structure–activity relationship; β-Asarone.
Subjects: Natural Product Chemistry
Depositing User: Dr. Aparna Maitra Pati
Date Deposited: 30 Dec 2011 03:21
Last Modified: 30 Dec 2011 03:21
URI: http://ihbt.csircentral.net/id/eprint/642

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