Bioorganic and Medicinal Chemistry Letters p. 1877 - 1880 (2010)
Update date:2022-08-02
Topics: Inhibitors Discovery Experimental Article SAR (Structure-Activity Relationship) Hydantoin
Yu, Wensheng
Guo, Zhuyan
Orth, Peter
Madison, Vincent
Chen, Lei
Dai, Chaoyang
Feltz, Robert J.
Girijavallabhan, Vinay M.
Kim, Seong Heon
Kozlowski, Joseph A.
Lavey, Brian J.
Li, Dansu
Lundell, Daniel
Niu, Xiaoda
Piwinski, John J.
Popovici-Muller, Janeta
Rizvi, Razia
Rosner, Kristin E.
Shankar, Bandarpalle B.
Shih, Neng-Yang
Arshad Siddiqui
Sun, Jing
Tong, Ling
Umland, Shelby
Wong, Michael K.C.
Yang, De-yi
Zhou, Guowei
We disclose inhibitors of TNF-α 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 d
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