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  • Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.

Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.

Bioorganic & medicinal chemistry letters (2006-01-24)
J I Levin, 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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Thiomorpholine, 98%