6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents

Chun Mao Lin, Sheng Tung Huang, Fu Wei Lee, Hsien-Saw Kuo, Mei Hsiang Lin

Research output: Contribution to journalArticlepeer-review

76 Citations (Scopus)


A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC50 value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.

Original languageEnglish
Pages (from-to)4402-4409
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number13
Publication statusPublished - Jul 1 2006


  • Anti-inflammation
  • Coumarin
  • ROS
  • iNOS

ASJC Scopus subject areas

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


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