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

Authors :
Arutyunyan AF
Kostyukov AA
Korolev SP
Gottikh MB
Kaluzhny DN
Susova OY
Zhuze AL
Source :
Molekuliarnaia biologiia [Mol Biol (Mosk)] 2023 May-Jun; Vol. 57 (3), pp. 517-527.
Publication Year :
2023

Abstract

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.

Details

Language :
Russian
ISSN :
0026-8984
Volume :
57
Issue :
3
Database :
MEDLINE
Journal :
Molekuliarnaia biologiia
Publication Type :
Academic Journal
Accession number :
37326056
Full Text :
https://doi.org/10.31857/S0026898423030023, EDN: CGXJLT