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Bioorg Med Chem Lett. 2006 May 15;16(10):2699-704. Epub 2006 Mar 3.

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

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. john.gilmore@bms.com

Abstract

A novel series of achiral TNF-alpha converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11nM in a porcine TACE assay and inhibited TNF-alpha production in an LPS-stimulated whole blood assay with an IC(50) value of 23nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases.

PMID:
16516466
DOI:
10.1016/j.bmcl.2006.02.015
[Indexed for MEDLINE]

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