Synthesis and structure–activity relationship of a novel, non-hydroxamate series of TNF-α converting enzyme inhibitors

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• 作者：John L. Gilmore ; Bryan W. King ; Naoyuki Asakawa ; Kimberly Harrison ; Andrew Tebben ; James E. Sheppeck II ; Rui-Qin Liu ; Maryanne Covington ; James J.-W. Duan
• 关键词：TACE ; Inflammation ; Rheumatoid arthritus
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 August 2007
• 年：2007
• 卷：17
• 期：16
• 页码：4678-4682
• 全文大小：286 K

文摘

A novel series of TNF-α converting enzyme (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds use a triazolethione moiety as the zinc binding ligand and exhibit IC₅₀ values from 1.5 to 100 nM in a porcine TACE assay. They also have excellent selectivities over other MMPs.