Broad spectrum matrix metalloproteinase inhibitors:: An examination of succinamide hydroxamate inhibitors with P1Cα gem-disubstitution

被引：10

作者：

Curtin, ML ^{[1
]}

Garland, RB ^{[1
]}

Davidsen, SK ^{[1
]}

Marcotte, PA ^{[1
]}

Albert, DH ^{[1
]}

Magoc, TJ ^{[1
]}

Hutchins, C ^{[1
]}

机构：

[1] Abbott Labs, Div Pharmaceut Prod, Canc Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(98)00255-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of P-1 C-alpha gem-disubstituted succinamide hydroxamate matrix metalloproteinase inhibitors were prepared stereoselectively and evaluated in vitro for their ability to inhibit MMP-1, MMP-2, and MMP-3. It was found that while methyl/allyl substitution as in 2 and 18 provided compounds that were broad spectrum inhibitors and nearly equipotent with parent inhibitor 1, a larger group such as bis-allyl as in 13 or gem-cyclopentyl as in 14 significantly reduced enzyme inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1443 / 1448

页数：6

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