Title of article
Discovery of novel hydroxamates as highly potent tumor necrosis factor-α converting enzyme inhibitors. Part II: Optimization of the S3′ pocket
Author/Authors
Robert D. Mazzola Jr.، نويسنده , , Zhaoning Zhu، نويسنده , , Lisa Sinning، نويسنده , , Brian McKittrick، نويسنده , , Brian Lavey، نويسنده , , James Spitler، نويسنده , , Joseph Kozlowski، نويسنده , , Shih Neng-Yang، نويسنده , , Guowei Zhou، نويسنده , , Zhuyan Guo، نويسنده , , Peter Orth، نويسنده , , Vincent Madison، نويسنده , , Jing Sun، نويسنده , , Daniel Lundell، نويسنده , , Xiaoda Niu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
5809
To page
5814
Abstract
A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, -2, -3, -7, -14, and ADAM-10. X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound to the enzyme in the S1′–S3′ pocket.
Keywords
TACE inhibitors , MMP inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800116
Link To Document