DNA sequence-specific ligands. XX. Synthesis, spectral properties, virological and biochemical studies of fluorescent dimeric trisbenzimidazoles DB3P(n)

Abstract

A new series of AT-speci c minor groove DNA ligands (DB 3 P(n); n = 1,2,3,4) were synthesized and their spectral, biological and virological properties were investigated in water media. The variable length of methylene spacer in middle of molecule structure allows to "recognize" sequences of blocks of three AT pairs located at different distances from each other. The biological trials have shown su cient capability to suppress activity of HIV-1 integrase catalytic activity at sub micromolar concentrations (0.25 -0.50 µМ). DB 3 P(n) were found as very effective inhibitor of simplex virus type I and DNA topoisomerase I. By confocal microscopy con rmed ability of compounds stain nuclei, that can be used as gene-expression regulator.