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  • Title: Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
    Author: Levin JI, Chen JM, Laakso LM, Du M, Schmid J, Xu W, Cummons T, Xu J, Jin G, Barone D, Skotnicki JS.
    Journal: Bioorg Med Chem Lett; 2006 Mar 15; 16(6):1605-9. PubMed ID: 16426848.
    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-alpha production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.
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