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

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

doi:10.1016/j.bmc.2007.09.014

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

Chun, Kwangwoo;
Park, Song-Kyu;
Kim, Hwan Mook;
Choi, Yongseok;
Kim, Myung-Hwa;
외 9명

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39

초록

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.

키워드

TNF-alpha converting enzyme (TACE); metalloproteinase-2 (MMP-2); metalloproteinase-9 (MMP-9); rheumatoid arthritis (RA); gelastatin hydroxamates; coumarin derivatives; NECROSIS-FACTOR-ALPHA; CATALYTIC DOMAIN; METALLOPROTEINASE; DISINTEGRIN

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

저자: 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

DOI: 10.1016/j.bmc.2007.09.014

발행일: 2008-01-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry

권: 16

호: 1

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