Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors |
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| Authors: | Gilmore John L King Bryan W Asakawa Naoyuki Harrison Kimberly Tebben Andrew Sheppeck James E Liu Rui-Qin Covington Maryanne Duan James J-W |
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| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. john.gilmore@bms.com |
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| Abstract: | A novel series of TNF-alpha converting enzyme (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds use a triazolethione moiety as the zinc binding ligand and exhibit IC50 values from 1.5 to 100 nM in a porcine TACE assay. They also have excellent selectivities over other MMPs. |
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