Synthesis and in vitro cytotoxicity of andrographolide-19-oic acid analogues as anti-cancer agents

被引：36

作者：

Chen, Dongsheng ^{[1
]}

Song, Yaping ^{[1
]}

Lu, Yunlong ^{[1
]}

Xue, Xiaowen ^{[1
]}

机构：

[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 11期

关键词：

Andrographolide; Structure modification; Andrographolide-19-oic acid derivatives; Cytotoxicity; ANDROGRAPHIS; ARREST; CELLS;

D O I：

10.1016/j.bmcl.2013.04.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a series of andrographolide-19-oic acid derivatives was described and their in vitro antitumor activity against two human cell lines was evaluated. Most compounds were found to exhibit significant cytotoxicity, better than andrographolide, and compounds 9d and 9b were identified as the most potent with IC50 values of 1.18 and 6.28 mu m against HCT-116 and MCF-7 cell lines, respectively. The preliminary results indicated that the oxidation of C-19-hydroxyl group of andrographolide to corresponding carboxyl group and the subsequent esterification of the formed carboxylic acid led to considerable improvement in cytotoxicity against the cancer cells. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：3166 / 3169

页数：4

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