Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1)

被引：24

作者：

Fray, MJ ^{[1
]}

Dickinson, RP ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(00)00720-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationships are described for a series of succinyl hydroxamic acids 4a-o as potent and selective inhibitors of matrix metalloprotease-3 (stromelysin-1). Optimisation of P1' and P3' groups gave compound 4j (MMP-3 IC50 = 5.9nM) which was >140-fold less potent against MMP-1 (IC50 = 51,000nM), MMP-2 (IC50=1790nM), MMP-9 (IC50 = 840 nM) and MMP-14 (IC50 = 1900 nM). (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：571 / 574

页数：4

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