Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors

Hee Ju Cho, Mi Ja Jung, Youngjoo Kwon, Younghwa Na

Research output: Contribution to journalArticlepeer-review

28 Scopus citations


A total of seven new oxyranylmethyloxy or thiiranylmethyloxy group substituted 5-azaxanthones and -acridones analogues were synthesized and tested for their biological activities for cancer cell lines and topoisomerases. Among the compounds, compound 5, 3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone, showed effective topoisomerase I inhibitory activity, 50% and 27% inhibition ratio at 100 and 20 μM, respectively. This result is the first finding of the function of 5-azaxanthone compounds for topoisomerase I inhibition and can provide a novel skeleton for the anticancer drug development process.

Original languageEnglish
Pages (from-to)6766-6769
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number23
StatePublished - 1 Dec 2009

Bibliographical note

Funding Information:
This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD) ( KRF-2006-521-E00159 ). M.-J. Jung was partially supported by the Brain Korea 21 project.


  • Acridone
  • Anticancer agents
  • Azaxanthone
  • Topoisomerase I inhibitor


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