Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation
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. (c) 2007 Elsevier Ltd. All rights reserved.
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Issue Date
- 2008-01
- Language
- English
- Article Type
- Article
- Keywords
NECROSIS-FACTOR-ALPHA; CATALYTIC DOMAIN; METALLOPROTEINASE; DISINTEGRIN
- Citation
BIOORGANIC MEDICINAL CHEMISTRY, v.16, no.1, pp.530 - 535
- ISSN
- 0968-0896
- Appears in Collection
- CH-Journal Papers(저널논문)
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