Title of article
Rational design, synthesis and structure–Activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 1: lead identification
Author/Authors
Chu-Biao Xue، نويسنده , , Xiaohua He، نويسنده , , John Roderick، نويسنده , , Ronald L. Corbett، نويسنده , , James J. -W. Duan، نويسنده , , Ruiqin Liu، نويسنده , , Maryanne B. Covington، نويسنده , , Robert C. Newton، نويسنده , , James M. Trzaskos، نويسنده , , Ronald L. Magolda، نويسنده , , Ruth R. Wexler، نويسنده , , Carl P. Decicco، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
5
From page
4293
To page
4297
Abstract
Rational design based on the broad spectrum MMP inhibitor CGS 27023A led to the identification of a novel series of cyclic succinate TACE inhibitors. As a mixture of two enantiomers, the lead compound 17b exhibited potent enzyme activity (IC50=8 nM) in the inhibition of porcine TNF-α converting enzyme (pTACE) and excellent selectivity over aggrecanase and MMP-1, -2 and -9.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793768
Link To Document