Substituted 2,5′-Bi-1H-benzimidazoles: Topoisoraerase I inhibition and cytotoxicity

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

Research output: Contribution to journalArticlepeer-review

251 Scopus citations


Several 2′-aryl-5-substituted-2,5′-bi-1H-benzimidazole derivatives were synthesized and evaluated as topoisomerase I poisons and for their cytotoxicity toward the human lymphoblast cell line RPMI 8402. This study focused on 18 2,5′-bi-1H-benzimidazole derivatives which contained either a 5-cyano, a 5-(aminocarbonyl), or a 5-(4-methylpiperazinyl) group. Among these bibenzimidazoles, the pharmacological activity of 2′-phenyl derivatives and the influence of the different positional isomers of either a 2′-tolyl group or a 2′-naphthyl moiety on cytotoxicity and topoisomerase I inhibitory activity were determined.

Original languageEnglish (US)
Pages (from-to)992-998
Number of pages7
JournalJournal of medicinal chemistry
Issue number4
StatePublished - Feb 16 1996

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


Dive into the research topics of 'Substituted 2,5′-Bi-1H-benzimidazoles: Topoisoraerase I inhibition and cytotoxicity'. Together they form a unique fingerprint.

Cite this