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Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation
- Authors
- Chun, Kwangwoo; Park, Song-Kyu; Kim, Hwan Mook; Choi, Yongseok; Kim, Myung-Hwa; Park, Chun-Ho; Joe, Bo-Young; Chun, Tae Gyu; Choi, Hyun-Moo; Lee, Hee-Yoon; Hong, Sung Hee; Kim, Myung Sook; Nam, Ky-Youb; Han, 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
- 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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