| Autor: |
Arutyunyan AF; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991 Russia., Kostyukov AA; Emanuel Institute of Biochemical Physics, Russian Academy of Science, Moscow, 119334 Russia., Korolev SP; Department of Chemistry, Moscow State University, Moscow, 119991 Russia.; Belozersky Institute of Physicochemical Biology, Moscow State University, Moscow, 119991 Russia., Gottikh MB; Department of Chemistry, Moscow State University, Moscow, 119991 Russia.; Belozersky Institute of Physicochemical Biology, Moscow State University, Moscow, 119991 Russia., Kaluzhny DN; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991 Russia., Susova OY; Research Institute of Carcinogenesis, Blokhin National Medical Research Center of Oncology, Moscow, 115478 Russia., Zhuze AL; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991 Russia.; zhuze@eimb.ru. |
| Abstrakt: |
In this work, we synthesized and characterized the properties of a series of new fluorescent DB3(n) narrow-groove ligands. DB3(n) compounds based on dimeric trisbenzimidazoles have the ability to bind to the AT regions of DNA. The synthesis of DB3(n), whose trisbenzimidazole fragments are linked by oligomethylene linkers of different lengths (n = 1, 5, 9), is based on the condensation of the MB3 monomeric trisbenzimidazole with α,ω-alkyldicarboxylic acids. DB3 (n) proved to be effective inhibitors of the catalytic activity of HIV-1 integrase at submicromolar concentrations (0.20-0.30 μM). DB3(n) was found to inhibit the catalytic activity of DNA topoisomerase I at low micromolar concentrations. |
