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. 2010 Mar 15;20(6):1877-80.
doi: 10.1016/j.bmcl.2010.01.148. Epub 2010 Feb 4.

Discovery and SAR of hydantoin TACE inhibitors

Wensheng Yu  1 , Zhuyan Guo, Peter Orth, Vincent Madison, Lei Chen, Chaoyang Dai, Robert J Feltz, Vinay M Girijavallabhan, Seong Heon Kim, Joseph A Kozlowski, Brian J Lavey, Dansu Li, Daniel Lundell, Xiaoda Niu, John J Piwinski, Janeta Popovici-Muller, Razia Rizvi, Kristin E Rosner, Bandarpalle B Shankar, Neng-Yang Shih, M Arshad Siddiqui, Jing Sun, Ling Tong, Shelby Umland, Michael K C Wong, De-yi Yang, Guowei Zhou
Affiliations

Discovery and SAR of hydantoin TACE inhibitors

Wensheng Yu et al. Bioorg Med Chem Lett. .

Abstract

We disclose inhibitors of TNF-alpha converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Crystal structures of inhibitors bound to TACE revealed monodentate coordination of the hydantoin to the zinc. SAR, X-ray, and modeling designs are described. To our knowledge, these are the first reported X-ray structures of TACE with a hydantoin zinc ligand.

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