Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation
- PMID: 17936631
- DOI: 10.1016/j.bmc.2007.09.014
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation
Abstract
A series of coumarin types MMP inhibitors were designed based on gelastatin hydroxamates (1) and evaluated for TACE, cellular TNF-alpha, and NO inhibitory activities. Among them, compounds 9b had potent inhibitory activities in enzymatic and cellular assays and good selectivity to MMP-2 and MMP-9. Further investigation of 9b will be carried out for its efficacy in RA animal model system.
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