Title of article :
Discovery of β-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors
Author/Authors :
James J. -W. Duan، نويسنده , , Lihua Chen، نويسنده , , Zhonghui Lu، نويسنده , , Chu-Biao Xue، نويسنده , , Ruiqin Liu، نويسنده , , Maryanne B. Covington، نويسنده , , Mingxin Qian، نويسنده , , Zelda R. Wasserman، نويسنده , , Krishna Vaddi، نويسنده , , David D. Christ، نويسنده , , James M. Trzaskos، نويسنده , , Robert C. Newton، نويسنده , , Carl P. Decicco، نويسنده ,
Abstract :
β-Benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and guiding SAR study. SAR optimization led to the discovery of compound 30 which met all in vitro and in vivo criteria for the program and was selected for further evaluation.
