Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases
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- 作者：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-Mul
- 关键词：Hydantoin ; TACE inhibitor ; Rheumatoid arthritis
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 December 2010
- 年：2010
- 卷：20
- 期：24
- 页码：7283-7287
- 全文大小：665 K
文摘
Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (Ki) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles.