Title of article
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates
Author/Authors
J.I. Levin، نويسنده , , J.M. Chen and Y.-C. Fang، نويسنده , , L.M. Laakso، نويسنده , , M. Du، نويسنده , , J. Schmid، نويسنده , , W. Xu، نويسنده , , T. Cummons، نويسنده , , J. Xu، نويسنده , , G. Jin، نويسنده , , D. Barone، نويسنده , , J.S. Skotnicki، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
1605
To page
1609
Abstract
A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1′ groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-α production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.
Keywords
Thiomorpholine , Sulfonamide: hydroxamate , rheumatoid arthritis , TACE inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796629
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