Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372115 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A novel series of TNF-α convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of l-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP’s. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.
Graphical abstractSynthesis and optimization of novel tartrate TACE inhibitors are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kristin E. Rosner, Zhuyan Guo, Peter Orth, Gerald W. Shipps Jr., David B. Belanger, Tin Yau Chan, Patrick J. Curran, Chaoyang Dai, Yongqi Deng, Vinay M. Girijavallabhan, Liwu Hong, Brian J. Lavey, Joe F. Lee, Dansu Li, Zhidan Liu, Janeta Popovici-Muller,