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Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation
- Authors
- Kwangwoo Chun ; Song-Kyu Park ; Hwan Mook Kim ; Yongseok Choi ; Myung-Hwa Kim ; Chun-Ho Park ; Bo-Young Joe ; Tae Gyu Chun ; Hyun-Moo Choi ; Hee-Yoon Lee ; Sung Hee Hong ; Myung Sook Kim ; Ky-Youb Nam ; Gyoonhee Han
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, Vol.16(1) : 530-535, 2008
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- ISSN
- 0968-0896
- Issue Date
- 2008
- MeSH
- ADAM Proteins/antagonists & inhibitors ; ADAM17 Protein ; Coumarins* ; Hydroxamic Acids ; Matrix Metalloproteinase Inhibitors ; Metalloendopeptidases/antagonists & inhibitors* ; Nitric Oxide/antagonists & inhibitors ; Protease Inhibitors/chemical synthesis* ; Protease Inhibitors/pharmacology ; Structure-Activity Relationship ; Tumor Necrosis Factor-alpha/antagonists & inhibitors
- Keywords
- TNF-a converting enzyme (TACE) ; Metalloproteinase-2(MMP-2) ; Metalloproteinase-9 (MMP-9) ; Rheumatoid arthritis (RA) ; Gelastatin hydroxamates ; Coumarin derivatives
- 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.
- Appears in Collections:
- 1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers
- Yonsei Authors
- Kim, Myung Hwa(김명화)
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