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

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

Bioorg Med Chem Lett ; 20(24): 7283-7, 2010 Dec 15.

Article in English | MEDLINE | ID: mdl-21106451

ABSTRACT

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.

Subject(s)

ADAM Proteins/antagonists & inhibitors , Anti-Inflammatory Agents/chemistry , Arthritis, Rheumatoid/drug therapy , Protease Inhibitors/chemistry , ADAM Proteins/metabolism , ADAM17 Protein , Acetylene/analogs & derivatives , Acetylene/pharmacokinetics , Acetylene/therapeutic use , Animals , Anti-Inflammatory Agents/pharmacokinetics , Anti-Inflammatory Agents/therapeutic use , Dogs , Haplorhini , Humans , Protease Inhibitors/pharmacokinetics , Protease Inhibitors/therapeutic use , Rats

ABSTRACT

Subject(s)

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