Synthesis and biological properties of benzo-annulated rutaecarpines

Young Hwan Hong, Woo Jin Lee, Seung Ho Lee, Jong Keun Son, Hye Lin Kim, Jung Min Nam, Youngjoo Kwon, Yurngdong Jahng

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


A series of benzo-annulated rutaecarpines were prepared from anthranilic acid and 3-aminonaphthalene-2- carboxylic acid by Fischer indole synthesis as key reaction. Cytotoxicity was somewhat increased by the introduction of benzo-annulation, which was not directly related to the inhibitory activity against topoisomerases (topo) I and II. Benzo-annulation on ring A led to significant increase of inhibitory activity against topo II while annulations on ring E increased inhibitory activity against topo I.

Original languageEnglish
Pages (from-to)1704-1709
Number of pages6
JournalBiological and Pharmaceutical Bulletin
Issue number10
StatePublished - 2010


  • Benzorutaecarpine
  • Cytotoxicity
  • Fischer indole synthesis
  • Rutaecarpine
  • Topoisomerase


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