Structure activity of topoisomerase i poisons related to hoechst 33342

Qun Sun, Barbra Gatto, Chiang Yu, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

Research output: Contribution to journalArticlepeer-review

57 Citations (Scopus)


A series of bisbenzimidazoles related to Hoechst 33342 were synthesized. Data on the relative activity of these bisbenzimidazoles as topoisomerase I poisons suggest that considerable flexibility exists in the location of the tertiary alkylamine moeity. With the exception of arylamine analogs, cytotoxicity was generally consistent with their relative potency as topoisomerase I poisons.

Original languageEnglish
Pages (from-to)2871-2876
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number24
Publication statusPublished - Dec 22 1994
Externally publishedYes

ASJC Scopus subject areas

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


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