DNA sequence-specific ligands. XX. Synthesis, spectral properties, virological and biochemical studies of fluorescent dimeric trisbenzimidazoles DB3P(n)статьяИсследовательская статья
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Аннотация:A new series of AT-specific minor groove DNA ligands (DB3P(n); n = 1,2,3,4) was synthesized and their spectral, biological and virological properties were investigated. With a methylene spacers of different lengths blocks of three AT pairs located at different distances from each other could be recognized. The compounds synthesized suppressed the activity of HIV-1 integrase at submicromolar concentrations (0.25–0.50 µМ). Also, DB3P(n) were found to be effective inhibitors of simplex virus type I and DNA topoisomerase I. The synthesized DB3P(n) demonstrated good solubility in water, could penetrate through cell and nuclear membranes, and stain DNA in live cells.