DNA sequence-specific ligands. XX. Synthesis, spectral properties, virological and biochemical studies of fluorescent dimeric trisbenzimidazoles DB 3 P(n)

A new series of AT-specific minor groove DNA ligands (DB 3 P( 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, DB 3 P( n ) were found to be effective inhibitors of simplex virus type I and DNA topoisomerase I. The synthesized DB 3 P( n ) demonstrated good solubility in water, could penetrate through cell and nuclear membranes, and stain DNA in live cells. Graphical Abstract