Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

Qun Sun, Barbara Gatto, Chiang Yu, Angela Liu, Leroy F. Liu, Edmond J. LaVoie

Research output: Contribution to journalArticlepeer-review

79 Citations (Scopus)


The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

Original languageEnglish
Pages (from-to)3638-3644
Number of pages7
JournalJournal of Medicinal Chemistry
Issue number18
Publication statusPublished - Sept 1 1995
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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