Synthesis, biological activity and comparative analysis of DNA binding affinities and human DNA topoisomerase I inhibitory activities of novel 12-alkoxy-benzo[c]phenanthridinium salts

Michael A Lynch, Olivier Duval, Alyona Sukhanova, Jerome Devy, Simon P MacKay, Roger D Waigh, Igor Nabiev

Research output: Contribution to journalArticle

80 Citations (Scopus)

Abstract

New antitumor 12-alkoxy-benzo[c]phenanthridinium derivatives were obtained in high yields through multistep syntheses. Analysis of DNA binding and human DNA topoisomerase I inhibitory activities demonstrates that new compounds, combining 2, 6, and 12 substitutions, interact strongly with DNA and exhibit important topoisomerase I inhibition. The cytotoxicities against solid tumor cell lines are also determined and compared with those for fagaronine and ethoxidine.

Original languageEnglish
Pages (from-to)2643-2646
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number19
Early online date20 Aug 2001
DOIs
Publication statusPublished - 8 Oct 2001

Keywords

  • naturally occurring alkaloids
  • biological activities
  • cytotoxicities
  • olid tumor cell lines

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