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Vol 57(2023) N 3 p. 512-521; DOI 10.1134/S0026893323030020  A.F. Arutyunyan1, A.A. Kostyukov2, S.P. Korolev3,4, M.B. Gottikh3,4, D.N. Kaluzhny1, O.Yu. Susova5, A.L. Zhuze1* DNA Sequence-Specific Ligands. 19. Synthesis, Spectral Properties, Virological and Biochemical Studies of DB3(n) Fluorescent Dimeric Trisbenzimidazoles 1Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991 Russia2Emanuel Institute of Biochemical Physics, Russian Academy of Science, Moscow, 119334 Russia 3Department of Chemistry, Moscow State University, Moscow, 119991 Russia 4Belozersky Institute of Physicochemical Biology, Moscow State University, Moscow, 119991 Russia 5Research Institute of Carcinogenesis, Blokhin National Medical Research Center of Oncology, Moscow, 115478 Russia *zhuze@eimb.ru Received - 2022-08-02; Revised - 2022-11-02; Accepted - 2022-11-03 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. DNA, sequence-specific minor-groove ligand, fluorescent dimeric trisbenzimidazoles DB3(n), spectral methods, HIV-1 integrase, DNA topoisomerase I |
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