| Literature DB >> 20663669 |
Wensheng Yu1, Ling Tong, Seong Heon Kim, Michael K C Wong, Lei Chen, De-Yi Yang, Bandarpalle B Shankar, Brian J Lavey, Guowei Zhou, Aneta Kosinski, Razia Rizvi, Dansu Li, Robert J Feltz, John J Piwinski, Kristin E Rosner, Neng-Yang Shih, M Arshad Siddiqui, Zhuyan Guo, Peter Orth, Himanshu Shah, Jing Sun, Shelby Umland, Daniel J Lundell, Xiaoda Niu, Joseph A Kozlowski.
Abstract
We disclose further optimization of hydantoin TNF-alpha convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds was shown to have sub-nanomolar K(i), good rat PK, and good selectivity versus MMP-1, -2, -3, -7, -9, and -13. Copyright 2010. Published by Elsevier Ltd.Entities:
Mesh：
Substances：
Year: 2010 PMID： 20663669 DOI： 10.1016/j.bmcl.2010.06.134
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823