2010•Biochemistry (Moscow)Requires access
Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I
Olga Yu. Susova, Anatoly A. Ivanov, Sandra Morales Ruiz, Ekaterina A. Lesovaya, A. V. Gromyko, Sergey A. Streltsov, Alexei L. Zhuze
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Abstract
The potential of six dimeric bisbenzimidazoles bound to scDNA to inhibit eukaryotic DNA topoisomerase (topo-I) was studied chemically; the tested compounds differed in linker structure and length. All the compounds inhibited topo-I, DB(7) being the most efficient; its inhibitory activity in vitro was 50-fold higher than that of camptothecin. It is noteworthy that inhibitory properties of nearly all the tested compounds increased many times if they were preincubated with scDNA for three days.