Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation
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- Title
- Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation
- Author(s)
- K Chun; Song Kyu Park; Hwan Mook Kim; Y Choi; M H Kim; C H Park; B Y Joe; T G Chun; H M Choi; H Y Lee; S H Hong; M S Kim; K Y Nam; G Han
- Bibliographic Citation
- Bioorganic & Medicinal Chemistry, vol. 16, no. 1, pp. 530-535
- Publication Year
- 2008
- Abstract
- A series of coumarin types MMP inhibitors were designed based on gelastatin hydroxamates (1) and evaluated for TACE, cellular TNF-α, 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.
- Keyword
- coumarin derivativesgelastatin hydroxamatesmetalloproteinase-2 (MMP-2)metalloproteinase-9 (MMP-9)rheumatoid arthritis (RA)TNF-α converting enzyme (TACE)
- ISSN
- 0968-0896
- Publisher
- Elsevier
- Full Text Link
- http://dx.doi.org/10.1016/j.bmc.2007.09.014
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
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