Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases

被引：39

作者：

Valente, Sergio ^{[1
]}

Bana, Emilie ^{[1
]}

Viry, Elodie ^{[1
]}

Bagrel, Denyse ^{[1
]}

Kirsch, Gilbert ^{[1
]}

机构：

[1] Univ Paul Verlaine, Lab Ingenierie Mol & Biochim Pharmacol, Inst Jean Barriol, FR CNRS 2843, F-57070 Metz, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 19期

关键词：

Cdc25; phosphatases; Coumarins; Chalcones; Heck coupling; CELL-GROWTH; SPECIFICITY;

D O I：

10.1016/j.bmcl.2010.07.130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5827 / 5830

页数：4

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