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

被引：64
|
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
收藏
页码：7426 / 7428
页数：3
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