Synthesis and structure-activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors

被引：32

作者：

Gilmore, JL ^{[1
]}

King, BW ^{[1
]}

Harris, C ^{[1
]}

Maduskuie, T ^{[1
]}

Mercer, SE ^{[1
]}

Liu, RQ ^{[1
]}

Covington, MB ^{[1
]}

Qian, MX ^{[1
]}

Ribadeneria, MD ^{[1
]}

Vaddi, K ^{[1
]}

Trzaskos, JM ^{[1
]}

Newton, RC ^{[1
]}

Decicco, CP ^{[1
]}

Duan, JJW ^{[1
]}

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ 08540 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

TACE inhibitors; metazincin; metalloprotease; sheddase; tumor necrosis factor; antiinflammatory; hydroxamic acid;

D O I：

10.1016/j.bmcl.2006.02.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of achiral TNF-alpha converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-alpha production in an LPS-stimulated whole blood assay with an IC50 value of 23 nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2699 / 2704

页数：6

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