Title of article
α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)
Author/Authors
Gregory R. Ott، نويسنده , , Naoyuki Asakawa، نويسنده , , Zhonghui Lu، نويسنده , , Ruiqin Liu، نويسنده , , Maryanne B. Covington، نويسنده , , Krishna Vaddi، نويسنده , , Mingxin Qian، نويسنده , , Robert C. Newton، نويسنده , , David D. Christ، نويسنده , , James M. Traskos، نويسنده , , Carl P. Decicco، نويسنده , , James J. -W. Duan، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
694
To page
699
Abstract
Selective inhibitors of TNF-α Converting Enzyme (TACE) based on (1R,2S)-cyclopentyl, (3S,4S)-pyrrolidinyl, and (3R,4S)-tetrahydrofuranyl β-benzamido hydroxamic acids have been synthesized and evaluated. This study has led to the discovery of novel inhibitors whose profiles include activity against TACE in an enzyme assay, potency in the suppression of LPS-stimulated TNF-α in human whole blood, selectivity against a panel of MMPs and oral bioavailability.
Keywords
TNF-? , Tumor necrosis factor-? converting enzyme , TACE , matrix metalloproteinase , ?-Amino acid , MMP
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799042
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