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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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39초록
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
- 발행일
- 2008-01-01
- 유형
- Article
- 권
- 16
- 호
- 1
- 페이지
- 530 ~ 535
- 언어
- ENG
- 출판사
- PERGAMON-ELSEVIER SCIENCE LTD
- 발행국가
- 영국
- 분량
- 6 페이지
- ISSN
- E 1464-3391
P 0968-0896