- Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.
Bioorganic & medicinal chemistry letters (2005-08-09)
J I Levin, J M Chen, L M Laakso, M Du, X Du, A M Venkatesan, V Sandanayaka, A Zask, J Xu, W Xu, Y Zhang, J S Skotnicki
PMID16084720
ZUSAMMENFASSUNG
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.
MATERIALIEN