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Article Doi

Discovery and SAR of hydantoin TACE inhibitors

DOI: 10.1016/j.bmcl.2010.01.148

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1877 - 1880 (2010)

Update date:2022-08-02

Topics: Inhibitors   Discovery   Experimental   Article   SAR (Structure-Activity Relationship)   Hydantoin  

Authors:

Yu, WenshengYu, Wensheng

Guo, ZhuyanGuo, Zhuyan

Orth, PeterOrth, Peter

Madison, VincentMadison, Vincent

Chen, LeiChen, Lei

Dai, ChaoyangDai, Chaoyang

Feltz, Robert J.Feltz, Robert J.

Girijavallabhan, Vinay M.Girijavallabhan, Vinay M.

Kim, Seong HeonKim, Seong Heon

Kozlowski, Joseph A.Kozlowski, Joseph A.

Lavey, Brian J.Lavey, Brian J.

Li, DansuLi, Dansu

Lundell, DanielLundell, Daniel

Niu, XiaodaNiu, Xiaoda

Piwinski, John J.Piwinski, John J.

Popovici-Muller, JanetaPopovici-Muller, Janeta

Rizvi, RaziaRizvi, Razia

Rosner, Kristin E.Rosner, Kristin E.

Shankar, Bandarpalle B.Shankar, Bandarpalle B.

Shih, Neng-YangShih, Neng-Yang

Arshad SiddiquiArshad Siddiqui

Sun, JingSun, Jing

Tong, LingTong, Ling

Umland, ShelbyUmland, Shelby

Wong, Michael K.C.Wong, Michael K.C.

Yang, De-yiYang, De-yi

Zhou, GuoweiZhou, Guowei

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Article abstract of DOI:10.1016/j.bmcl.2010.01.148

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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Full text of DOI:10.1016/j.bmcl.2010.01.148

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