1.
Bioorg Med Chem Lett
; 13(16): 2799-803, 2003 Aug 18.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12873518
RESUMO
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, all bearing a butynyloxy P1' group, was explored. In particular, compound 5j has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and MMP-9, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.