Abstract
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1′ groups was explored. In particular, compound 4t bearing a butynyloxy P1′ moiety has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and oral activity in an in vivo model of TNF-α production.
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