Anthranilate sulfonamide hydroxamate TACE inhibitors.: Part 2:: SAR of the acetylenic P1′ group

被引：71

作者：

Levin, JI

Chen, JM

Du, MT

Nelson, FC

Killar, LM

Skala, S

Sung, A

Jin, G

Cowling, R

Barone, D

March, CJ

Mohler, KM

Black, RA

Skotnicki, JS

机构：

[1] Wyeth Ayerst Res, Pearl River, NY 10965 USA

[2] Wyeth Ayerst Res, Princeton, NJ 08543 USA

[3] Immunex Res & Dev Corp, Seattle, WA 98101 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(02)00136-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1' groups was explored. In particular, compound 4t bearing a butynylox P1' moiety has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and oral activity in an in vitro model of TNF-alpha production. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1199 / 1202

页数：4

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