Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases

✍ Scribed by Vinay M. Girijavallabhan; Lei Chen; Chaoyang Dai; Robert J. Feltz; Luke Firmansjah; Dansu Li; Seong Heon Kim; Joseph A. Kozlowski; Brian J. Lavey; Aneta Kosinski; John J. Piwinski; Janeta Popovici-Muller; Razia Rizvi; Kristin E. Rosner; Banderpalle B. Shankar; Neng-Yang Shih; M. Arshad Siddiqui; Ling Tong; Michael K.C. Wong; De-yi Yang; Liping Yang; Wensheng Yu; Guowei Zhou; Zhuyan Guo; Peter Orth; Vincent Madison; Hong Bian; Daniel Lundell; Xiaoda Niu; Himanshu Shah; Jing Sun; Shelby Umland

• Book ID: 104005038
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 666 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.10.081

✦ Synopsis

Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles.