Author/Authors :
J.I. Levin، نويسنده , , J.M. Chen and Y.-C. Fang، نويسنده , , L.M. Laakso، نويسنده , , M. Du، نويسنده , , X. Du، نويسنده , , A.M. Venkatesan، نويسنده , , V. Sandanayaka، نويسنده , , A. Zask، نويسنده , , J. Xu، نويسنده , , W. Xu، نويسنده , , Y. Zhang، نويسنده , , J.S. Skotnicki، نويسنده ,
Abstract :
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-α production and a collagen-induced arthritis model.
Keywords :
TACE , MMP , Hydroxamate , rheumatoid arthritis
