Metadata of CSIR Papers
View Archive Info| Field | Value | |
| Creator |
Kumar, R
Mohanakrishnan, D Sharma, A Kaushik, NK Kalia, K Sinha, AK Sahal, D |
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| Subject |
Pharmacology & Pharmacy
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| Description |
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 beta-asarone rich Acorns calamus oil. Cytotoxic evaluation indicated that the most active compounds 27 (IC(50): 1.8 mu M) and 26 (IC(50): 2 mu M) were also relatively non-toxic. Furthermore, compound 12 showed excellent resistance index of 1.1 against chloroquine resistant Dd2 strain of P. falciparum. (C) 2010 Elsevier Masson SAS. All rights reserved.
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| Publisher |
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIERPARIS23 RUE LINOIS, 75724 PARIS, FRANCE
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| Date |
2011-09-20T12:08:54Z
2011-09-20T12:08:54Z 2010 |
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| Type |
Article
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| Identifier |
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
0223-5234 http://hdl.handle.net/123456789/13552 |
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| Language |
English
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