Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation

Cited 31 time in scopus
Metadata Downloads
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
DOI
http://dx.doi.org/10.1016/j.bmc.2007.09.014
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
Files in This Item:
  • There are no files associated with this item.


Items in OpenAccess@KRIBB are protected by copyright, with all rights reserved, unless otherwise indicated.