Bioorganic & Medicinal Chemistry Letters 2000-04-17

Heterocyclic bibenzimidazole derivatives as topoisomerase I inhibitors.

S Jin, J S Kim, S P Sim, A Liu, D S Pilch, L F Liu, E J LaVoie

Index: Bioorg. Med. Chem. Lett. 10 , 719, (2000)

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Abstract

A series of 2'-heterocyclic derivatives of 5-phenyl-2,5'-1H-bibenzimidazoles were evaluated for topoisomerase I poisoning activity and cytotoxicity. Topo I poisoning activity was associated with 2'-derivatives that possessed a hydrogen atom capable of hydrogen bond formation, suggesting that the interatomic distances between such hydrogen atoms and the heteroatoms on the adjacent benzimidazole influence activity.