Bioorganic & Medicinal Chemistry Letters 2011-05-15

Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitors.

Rahul Balasaheb Aher, Gajanan Wanare, Neha Kawathekar, Ravi Ranjan Kumar, Naveen Kumar Kaushik, Dinkar Sahal, Virander Singh Chauhan

文献索引：Bioorg. Med. Chem. Lett. 21 , 3034-6, (2011)

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摘要

A series of dibenzylideneacetones (A1-A12) and some of their pyrazolines (B1-B4) were synthesized and evaluated in vitro for blood stage antiplasmodial properties in Plasmodium falciparum culture using SYBR-green-I fluorescence assay. The compound (1E, 4E)-1,5-bis(3,4-dimethoxyphenyl)penta-1,4-dien-3-one (A9) was found to be the most active with IC(50) of 1.97 μM against chloroquine-sensitive strain (3D7) and 1.69 μM against chloroquine-resistant field isolate (RKL9). The MTT based cytotoxicity assay on HeLa cell line has confirmed that A9 is selective in its action against malaria parasite (with a therapeutic index of 166). Our results revealed that these compounds exhibited promising antiplasmodial activities which can be further explored as potential leads for the development of cheaper, safe, effective and potent drugs against chloroquine-resistant malarial parasites.Copyright © 2011. Published by Elsevier Ltd.