Synthesis, cytotoxicity and topoisomerase II inhibitory activity of benzonaphthofurandiones

Hee Kyung Rhee, Youngjoo Kwon, Hwa Jin Chung, Sang Kook Lee, Hea Young Park Choo

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


Benzonaphthofurandiones containing four coplanar fused aromatic rings were synthesized and evaluated for their cytotoxicity against five human cancer cell lines, and their inhibitory activity on topoisomerases. These benzonaphthofurandiones were prepared by condensation of 2,3- dichloronaphthoquinone and three aromatic diols with base catalysts in alcohol. The synthesized compounds were o-alkylated with six dialkylaminoalkyl halides. The hydroxy derivatives (8a-8g) exhibited relatively potent cytotoxicity among the prepared compounds. These compounds were evaluated as excellent inhibitors against topoisomerase II (topo II). Especially, the hydroxy analogue with branched methyl side chain (8e) showed high cytotoxicity against cancer cell lines and good inhibitory activity on topo II.

Original languageEnglish
Pages (from-to)2391-2396
Number of pages6
JournalBulletin of the Korean Chemical Society
Issue number7
StatePublished - 20 Jul 2011


  • Benzonaphthofurandiones
  • Cytotoxicity
  • Topoisomerase II


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