1. Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation
- Author
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Yongseok Choi, Song Kyu Park, Gyoonhee Han, Bo Young Joe, Kwangwoo Chun, Sung Hee Hong, Hyun Moo Choi, Hwan Mook Kim, Tae Gyu Chun, Myung Hwa Kim, Hee-Yoon Lee, Chun Ho Park, Myung Sook Kim, and Ky Youb Nam
- Subjects
Matrix metalloproteinase inhibitor ,medicine.medical_treatment ,Clinical Biochemistry ,Pharmaceutical Science ,ADAM17 Protein ,Matrix Metalloproteinase Inhibitors ,Hydroxamic Acids ,Nitric Oxide ,Biochemistry ,Chemical synthesis ,Structure-Activity Relationship ,chemistry.chemical_compound ,Coumarins ,Drug Discovery ,medicine ,Protease Inhibitors ,Molecular Biology ,chemistry.chemical_classification ,Hydroxamic acid ,biology ,Tumor Necrosis Factor-alpha ,Organic Chemistry ,Metalloendopeptidases ,Coumarin ,In vitro ,ADAM Proteins ,Enzyme ,Cytokine ,chemistry ,Enzyme inhibitor ,biology.protein ,Molecular Medicine - Abstract
A series of coumarin types MMP inhibitors were designed based on gelastatin hydroxamates (1) and evaluated for TACE, cellular TNF-α, 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.
- Published
- 2008
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