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

Authors
Chun, KwangwooPark, Song-KyuKim, Hwan MookChoi, YongseokKim, Myung-HwaPark, Chun-HoJoe, Bo-YoungChun, Tae GyuChoi, Hyun-MooLee, Hee-YoonHong, Sung HeeKim, Myung SookNam, Ky-YoubHan, Gyoonhee
Issue Date
1-1월-2008
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
TNF-alpha converting enzyme (TACE); metalloproteinase-2 (MMP-2); metalloproteinase-9 (MMP-9); rheumatoid arthritis (RA); gelastatin hydroxamates; coumarin derivatives
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.16, no.1, pp.530 - 535
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
Volume
16
Number
1
Start Page
530
End Page
535
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/124452
DOI
10.1016/j.bmc.2007.09.014
ISSN
0968-0896
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. (c) 2007 Elsevier Ltd. All rights reserved.
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