Anti-HBV and cytotoxic activities of pyranocoumarin derivatives

Chung Ren Su, Sheau Farn Yeh, Chih Miem Liu, Amooru G. Damu, Tsung Hsiao Kuo, Po Cheng Chiang, Kenneth F. Bastow, Kuo Hsiung Lee, Tian Shung Wu

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99 Citations (Scopus)


Four natural pyranocoumarins clausenidin (1), nordentatin (2), clausarin (3), and xanthoxyletin (4) were isolated from the medicinal plant Clausena excavata. Recently, we found that 1 and 2 suppressed hepatitis B virus surface antigen in HepA2 cells, and in addition, 1-3 showed cytotoxic activity against four human cancer cell lines (A549, MCF7, KB, and KB-VIN). To explore the SAR of 1-4, 17 pyranocoumarin analogues (5-21) were designed and synthesized. Among these analogues, 5 and 10 were the most potent against hepatitis B virus with EC50 values of 1.14 and 1.34 μM, respectively. The most interesting result in the cytotoxicity assay was the significant activity of 1, 5, and 6 against the multi-drug resistant cell line, KB-VIN, without activity against the KB cell line. These data suggest that these three compounds could be useful hits for developing MDR-inverse drugs.

Original languageEnglish
Pages (from-to)6137-6143
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number16
Publication statusPublished - 2009 Aug 15

All Science Journal Classification (ASJC) codes

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


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