Improved gelatinase A selectivity by novel zinc binding groups containing galardin derivatives

被引：65

作者：

Augé, F

Hornebeck, W

Decarme, M

Laronze, JY

机构：

[1] Univ Reims, Fac Pharm, IFR Biomol 53, UMR 6013, F-51096 Reims, France

[2] Univ Reims, Fac Med, IFR Biomol 53, CNRS,FRE 2534, F-51096 Reims, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(03)00214-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of several analogues of galardin, a MMP inhibitor, are presented with their in vitro inhibitory activity against MMP-1 and MMP-2. These compounds contain a distinct Zinc Binding Group (ZBG). Those having a 2-acylated-heterocycle as well as a 2-arylamide function do not exhibit a good inhibition/selectivity against the enzymes tested. On the contrary, those that are based on a hydrazide scaffold present potent selectivity for MMP-2 versus MMP-1. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1783 / 1786

页数：4

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