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  • Title: Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.
    Author: Chun K, Park SK, Kim HM, Choi Y, Kim MH, Park CH, Joe BY, Chun TG, Choi HM, Lee HY, Hong SH, Kim MS, Nam KY, Han G.
    Journal: Bioorg Med Chem; 2008 Jan 01; 16(1):530-5. PubMed ID: 17936631.
    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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