| Literature DB >> 21458257 |
Chaoyang Dai1, Dansu Li, Janeta Popovici-Muller, Lianyun Zhao, Vinay M Girijavallabhan, Kristin E Rosner, Brian J Lavey, Razia Rizvi, Bandarpalle B Shankar, Michael K C Wong, Zhuyan Guo, Peter Orth, Corey O Strickland, Jing Sun, Xiaoda Niu, Shiying Chen, Joseph A Kozlowski, Daniel J Lundell, John J Piwinski, Neng-Yang Shih, M Arshad Siddiqui.
Abstract
TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.Entities:
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Year: 2011 PMID： 21458257 DOI： 10.1016/j.bmcl.2011.01.002
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823