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 journalArticle

29 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 languageEnglish
Pages (from-to)530-535
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number1
DOIs
Publication statusPublished - 2008 Jan 1

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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    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