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

Department of Biotechnology

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.

Keywords

Coumarin derivatives
Gelastatin hydroxamates
Metalloproteinase-2 (MMP-2)
Metalloproteinase-9 (MMP-9)
Rheumatoid arthritis (RA)
TNF-α converting enzyme (TACE)

ASJC Scopus subject areas

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.",

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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

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AU - Lee, Hee Yoon

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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

Keywords

ASJC Scopus subject areas

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