Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

被引：13
|
作者：
Lombart, Henry-Georges
Feyfant, Eric
Joseph-McCarthy, Diane
Huang, Adrian
Lovering, Frank
Sun, LinHong
Zhu, Yi
Zeng, Congmei
Zhang, Yuhua
Levin, Jeremy
机构：
[1] Wyeth Res, Chem & Screening Sci, Cambridge, MA 02140 USA
[2] Wyeth Res, Chem & Screening Sci, Pearl River, NY 10965 USA
[3] Wyeth Res, Inflammat, Cambridge, MA 02140 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期
关键词：
inflammation; TACE; rheumatoid arthritis;
D O I：
10.1016/j.bmcl.2007.05.022
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-based methods were used to design P-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based assays. These analogs exhibit excellent in vitro potency against isolated TACE enzyme and show good selectivity for TACE over the related metalloproteases MMP-2, -13, and -14. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4333 / 4337
页数：5
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