Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
作者信息
Guo Zhuyan, Orth Peter, Wong Shing-Chun, Lavey Brian J, Shih Neng-Yang, Niu Xiaoda, Lundell Daniel J, Madison Vincent, Kozlowski Joseph A
机构信息
Department of Chemistry, Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
出版信息
Bioorg Med Chem Lett. 2009 Jan 1;19(1):54-7. doi: 10.1016/j.bmcl.2008.11.034. Epub 2008 Nov 14.
PMID:19054672
Abstract
We have discovered nanomolar inhibitors of TNF-alpha convertase (TACE) comprised of a novel spirocyclic scaffold and either a carboxylate or hydroxamate zinc binding moiety. X-ray crystal structures and computer models of selected compounds binding to TACE explain the observed SAR. We report the first TACE X-ray crystal structure for an inhibitor with a carboxylate zinc ligand.
摘要
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