| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361982 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chaoyang Dai, Dansu Li, Janeta Popovici-Muller, Lianyun Zhao, Vinay M. Girijavallabhan, Kristin E. Rosner, Brian J. Lavey, Razia Rizvi, Bandarpalle B. Shankar, Michael K.C. Wong, Zhuyan Guo, Peter Orth, Corey O. Strickland, Jing Sun, Xiaoda Niu,