Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group |
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| Authors: | Levin J I Chen J M Du M T Nelson F C Killar L M Skala S Sung A Jin G Cowling R Barone D March C J Mohler K M Black R A Skotnicki J S |
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| Affiliation: | Wyeth-Ayerst Research, 401N. Middletown Road, Pearl River, NY 10965, USA. levinj@war.wyeth.com |
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| 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-alpha production. |
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