Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors

Won Jea Cho, Quynh Manh Le, Hue Thi My Van, Kwang Youl Lee, Bok Yun Kang, Eung Seok Lee, Sang Kook Lee, Youngjoo Kwon

Research output: Contribution to journalArticlepeer-review

47 Scopus citations

Abstract

An intramolecular radical cyclization reaction of 4-bromo-3-arylisoquinolines 11a-c allowed the efficient synthesis of 11-methylindenoisoquinolines 2a-c. 5-(2-Aminoethylamino)indeno[1,2-c]isoquinolin-11-one 4 was also prepared in the convenient manner. The synthesized compounds were tested in vitro for cytotoxicity and DNA-topoisomerase 1 (top 1) inhibitory activity. The dramatic enhancement of top 1 inhibitory activity of 4 was explained by a docking study using the FlexX program.

Original languageEnglish
Pages (from-to)3531-3534
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number13
DOIs
StatePublished - 1 Jul 2007

Keywords

  • Antitumor agents
  • Docking study
  • FlexX
  • Indeno[1,2-c]isoquinolines
  • Synthesis of isoquinolines
  • Topoisomerase 1 inhibitor

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