| Literature DB >> 16426848 |
J I Levin1, J M Chen, L M Laakso, M Du, J Schmid, W Xu, T Cummons, J Xu, G Jin, D Barone, J S Skotnicki.
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.Entities:
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Year: 2006 PMID： 16426848 DOI： 10.1016/j.bmcl.2005.12.020
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823