DNA Sequence-Specific Ligands. 19. Synthesis, Spectral Properties, Virological and Biochemical Studies of DB3(n) Fluorescent Dimeric Trisbenzimidazoles

被引：0
作者：
A. F. Arutyunyan
A. A. Kostyukov
S. P. Korolev
M. B. Gottikh
D. N. Kaluzhny
O. Yu. Susova
A. L. Zhuze
机构：
[1] Engelhardt Institute of Molecular Biology,
[2] Russian Academy of Sciences,undefined
[3] Emanuel Institute of Biochemical Physics,undefined
[4] Russian Academy of Science,undefined
[5] Department of Chemistry,undefined
[6] Moscow State University,undefined
[7] Belozersky Institute of Physicochemical Biology,undefined
[8] Moscow State University,undefined
[9] Research Institute of Carcinogenesis,undefined
[10] Blokhin National Medical Research Center of Oncology,undefined
来源：
Molecular Biology | 2023年 / 57卷
关键词：
DNA; sequence-specific minor-groove ligand; fluorescent dimeric trisbenzimidazoles ; (; ); spectral methods; HIV-1 integrase; DNA topoisomerase I;
D O I：
暂无
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学科分类号：
摘要：
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.
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页码：512 / 521
页数：9
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