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Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. doi: 10.1016/j.bmcl.2008.09.045. Epub 2008 Sep 13.

Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.

Author information

1
Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA. robert.mazzola@spcorp.com

Abstract

A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, -2, -3, -7, -14, and ADAM-10. X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound to the enzyme in the S1'-S3' pocket.

PMID:
18835710
DOI:
10.1016/j.bmcl.2008.09.045
[Indexed for MEDLINE]

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