Synthesis and in vitro evaluation of novel coumarin-chalcone hybrids as potential anticancer agents

被引:259
|
作者
Sashidhara, Koneni V. [1 ]
Kumar, Abdhesh [1 ]
Kumar, Manoj [1 ]
Sarkar, Jayanta [2 ]
Sinha, Sudhir [2 ]
机构
[1] Cent Drug Res Inst CDRI CSIR, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst CDRI CSIR, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India
关键词
Synthesis; Coumarin; Chalcone; In vitro; Cytotoxicity; BIOLOGICAL EVALUATION; ANALOGS; DESIGN; DERIVATIVES;
D O I
10.1016/j.bmcl.2010.10.116
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of coumarin-chalcone hybrids have been synthesized and evaluated for their in vitro cytotoxicity against a panel of four human cancer cell lines and normal fibroblasts (NIH3T3). Among 21 compounds screened, three compounds (23, 25 and 26) showed IC50 range from 3.59 to 8.12 mu M. The most promising compound 26 showed around 30-fold more selectivity towards C33A (cervical carcinoma) cells over normal fibroblast NIH3T3 cells with an IC50 value of 3.59 mu M. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7205 / 7211
页数:7
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