Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. Issue 14 (15th July 2017)

• Record Type: Journal Article
• Authors: Tong, Ling; Kim, Seong Heon; Rosner, Kristin; Yu, Wensheng; Shankar, Bandarpalle B.; Chen, Lei; Li, Dansu; Dai, Chaoyang; Girijavallabhan, Vinay; Popovici-Muller, Janeta; Yang, Liping; Zhou, Guowei; Kosinski, Aneta; Siddiqui, M. Arshad; Shih, Neng-Yang; Guo, Zhuyan; Orth, Peter; Chen, Shiying; Lundell, Daniel; Niu, Xiaoda; Umland, Shelby; Kozlowski, Joseph A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 14(2017)
• Page Start: 3037
• Page End: 3042
• Publication Date: 2017-07-15
• Subjects: Tumor necrosis factor-alpha -- TACE inhibitors -- Hydantoin; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.05.062
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series.