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

被引：29

作者：

Chun, Kwangwoo ^{[1
,4
]}

Park, Song-Kyu ^{[2
]}

Kim, Hwan Mook ^{[2
]}

Choi, Yongseok ^{[3
,5
]}

Kim, Myung-Hwa ^{[4
]}

Park, Chun-Ho ^{[4
]}

Joe, Bo-Young ^{[4
]}

Chun, Tae Gyu ^{[1
,5
]}

Choi, Hyun-Moo ^{[5
]}

Lee, Hee-Yoon ^{[5
]}

Hong, Sung Hee ^{[1
]}

Kim, Myung Sook ^{[1
]}

Nam, Ky-Youb ^{[6
]}

Han, Gyoonhee ^{[1
]}

机构：

[1] Yonsei Univ, Dept Biotechnol, Seoul 120740, South Korea

[2] Korea Res Inst Biosci & Biotechnol, Taejon 305806, South Korea

[3] Korea Univ, Sch Biosci & Biotechnol, Seoul 136713, South Korea

[4] Jeil Pharmaceut Co, Seoul, South Korea

[5] Korea Adv Inst Sci & Technol, Dept Chem, Taejon 305701, South Korea

[6] BMDRC, Yonsei Engn Res Complex, Seoul 1207401, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 01期

关键词：

TNF-alpha converting enzyme (TACE); metalloproteinase-2 (MMP-2); metalloproteinase-9 (MMP-9); rheumatoid arthritis (RA); gelastatin hydroxamates; coumarin derivatives;

D O I：

10.1016/j.bmc.2007.09.014

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：530 / 535

页数：6

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