Minor groove dimeric bisbenzimidazoles inhibit in vitro DNA binding to eukaryotic DNA topoisomerase I.
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.
Susova
O Yu
OY
Blokhin Cancer Research Center, Russian Academy of Medical Sciences, Moscow, Russia. susovaolga@gmail.com
Ivanov
A A
AA
Morales Ruiz
S S
SS
Lesovaya
E A
EA
Gromyko
A V
AV
Streltsov
S A
SA
Zhuze
A L
AL
D006690:Bisbenzimidazole / Q000737:chemistry / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D019281:Dimerization; D011485:Protein Binding; D059004:Topoisomerase I Inhibitors
D059004:Topoisomerase I Inhibitors; D004247:DNA; D004264:DNA Topoisomerases, Type I; D006690:Bisbenzimidazole