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Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation |
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| Authors: | 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 |
| Affiliation: | Department of Biotechnology, Yonsei University, Seodaemun-gu, Seoul 120-740, Republic of Korea. |
| 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. |
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