Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates

被引：49

作者：

Levin, JI

Chen, JM

Laakso, LM

Du, M

Du, X

Venkatesan, AM

Sandanayaka, V

Zask, A

Xu, J

Xu, W

Zhang, Y

Skotnicki, JS

机构：

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

[2] Wyeth Res, Cambridge, MA 02140 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

TACE; MMP; hydroxamate; rheumatoid arthritis;

D O I：

10.1016/j.bmcl.2005.06.072

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 a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TALE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model. (c) 2005 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4345 / 4349

页数：5

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