Discovery of novel osthole derivatives as potential anti-breast cancer treatment

被引：65

作者：

You, Lisha ^{[1
]}

An, Rui ^{[1
]}

Wang, Xinhong ^{[1
]}

Li, Yimin ^{[1
]}

机构：

[1] Shanghai Univ Tradit Chinese Med, Sch Tradit Chinese Pharm, Shanghai 201203, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 24期

关键词：

Osthole; Antitumor; Breast cancer; Natural product; Structure modification; COUMARIN DERIVATIVES; PREVENTION;

D O I：

10.1016/j.bmcl.2010.10.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Osthole, an ingredient of Traditional Chinese Medicine (TCM) from natural product Cnidium monnieri (L.) Cusson, was used as a lead compound for structural modification. A series of osthole derivatives bearing aryl substituents at 3-position of coumarin, has been prepared and evaluated for their growth inhibitory activity against human breast cancer cell lines MCF-7 and MDA-MB-231. Interestingly, some derivatives exhibited good inhibition, among them compound 8e was found to be the most potent compound with IC50 values of 0.24 mu M, 0.31 mu M against MCF-7 and MDA-MB-231, respectively, which was improved more than 100-folds compared with its parent compound osthole. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7426 / 7428

页数：3

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