Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates |
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| Authors: | Levin J I Chen J M Laakso L M Du M Du X Venkatesan A M Sandanayaka V Zask A Xu J Xu W Zhang Y Skotnicki J S |
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| Institution: | Wyeth Research, 401N. Middletown Road, Pearl River, NY 10965, USA. levinji@wyeth.com |
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| 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-alpha production and a collagen-induced arthritis model. |
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