Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket |
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| Authors: | Huang Adrian Joseph-McCarthy Diane Lovering Frank Sun Linhong Wang Weiheng Xu Weixin Zhu Yi Cui Junqing Zhang Yuhua Levin Jeremy I |
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| Affiliation: | Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Drive, Cambridge, MA 02140, USA. ahuang@wyeth.com |
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| Abstract: | A series of beta-sulfonyl hydroxamate TACE inhibitors, bearing a butynylamino or a butynyloxy P1' group, was designed and synthesized. Of the compounds investigated, 22 has excellent potency against isolated TACE enzyme, shows good selectivity over MMP-2 and MMP-13, and oral activity in an in vivo mouse model of TNF-alpha production. |
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