Article ID Journal Published Year Pages File Type
1379600 Bioorganic & Medicinal Chemistry Letters 2005 5 Pages PDF
Abstract

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 TACE enzyme and in cells, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.

Graphical abstractThe 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 TACE enzyme and in cells, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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