| Autor: |
Levin JI; Wyeth Research, 401 N Middletown Rd, Pearl River, NY 10965, USA. levinji@wyeth.com, Chen JM, Cheung K, Cole D, Crago C, Santos ED, Du X, Khafizova G, MacEwan G, Niu C, Salaski EJ, Zask A, Cummons T, Sung A, Xu J, Zhang Y, Xu W, Ayral-Kaloustian S, Jin G, Cowling R, Barone D, Mohler KM, Black RA, Skotnicki JS |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Aug 18; Vol. 13 (16), pp. 2799-803. |
| DOI: |
10.1016/s0960-894x(03)00514-6 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect