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

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

doi:10.1016/j.bmc.2007.09.014

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

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

Research output: Contribution to journal › Article › peer-review

35 Citations (Scopus)

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.

Original language	English
Pages (from-to)	530-535
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	16
Issue number	1
DOIs	https://doi.org/10.1016/j.bmc.2007.09.014
Publication status	Published - 2008 Jan 1

Bibliographical note

Funding Information:
This research was supported by Seoul R&BD Program (10541), a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Welfare, and the Brain Korea 21 project the Republic of Korea.

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2007.09.014

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Chun, K., Park, S. K., Kim, H. M., Choi, Y., Kim, M. H., Park, C. H., Joe, B. Y., Chun, T. G., Choi, H. M., Lee, H. Y., Hong, S. H., Kim, M. S., Nam, K. Y., & Han, G. (2008). Chromen-based TNF-α converting enzyme (TACE) inhibitors: Design, synthesis, and biological evaluation. Bioorganic and Medicinal Chemistry, 16(1), 530-535. https://doi.org/10.1016/j.bmc.2007.09.014

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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.",

author = "Kwangwoo Chun and Park, {Song Kyu} and Kim, {Hwan Mook} and Yongseok Choi and Kim, {Myung Hwa} and Park, {Chun Ho} and Joe, {Bo Young} and Chun, {Tae Gyu} and Choi, {Hyun Moo} and Lee, {Hee Yoon} and Hong, {Sung Hee} and Kim, {Myung Sook} and Nam, {Ky Youb} and Gyoonhee Han",

note = "Funding Information: This research was supported by Seoul R&BD Program (10541), a Grant (0405-NS01-0704-0001) of the Korean Health 21 R&D Project, Ministry of Health and Welfare, and the Brain Korea 21 project the Republic of Korea.",

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AU - Choi, Yongseok

AU - Kim, Myung Hwa

AU - Park, Chun Ho

AU - Joe, Bo Young

AU - Chun, Tae Gyu

AU - Choi, Hyun Moo

AU - Lee, Hee Yoon

AU - Hong, Sung Hee

AU - Kim, Myung Sook

AU - Nam, Ky Youb

AU - Han, Gyoonhee

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

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

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