Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex

H. T M Van, Quynh Manh Le, Kwang Youl Lee, Eung Seok Lee, Youngjoo Kwon, Tae Sung Kim, Thanh Nguyen Le, Suh H. Lee, Won J. Cho

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29 Citations (Scopus)


11-Hydroxyindeno[1,2-c]isoquinolines 12a-c were prepared as constrained forms of 3-arylisoquinolines through an intramolecular cyclization reaction. Among the synthesized compounds, the 11-ibutoxy analog 15l displayed potent in vitro cytotoxicity against four different tumor cell lines as well as topoisomerase 1 inhibitory activity. A FlexX docking study was performed to explain the topoisomerase 1 activity of 15l.

Original languageEnglish
Pages (from-to)5763-5767
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number21
Publication statusPublished - 2007 Nov 1



  • Antitumor agents
  • Cytotoxicity
  • Docking study
  • Indenoisoquinoline
  • Synthesis
  • Topoisomerase 1

ASJC Scopus subject areas

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

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