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DNA sequence-specific ligands. XVII. Synthesis,spectral properties,virological and biochemical studies of fluorescent dimeric bisbenzimidazoles DBA(n) |
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| Authors: | Vasiliy S. Koval Albert F. Arutyunyan Victor L. Salyanov Regina R. Klimova Alla A. Kushch Ekaterina Yu. Rybalkina Olga Yu. Susova Alexei L. Zhuze |
| Affiliation: | 1. Engelhardt Institute of Molecular Biology Russian Academy of Sciences, Vavilova St. 32, Moscow 119991, Russia;2. Ivanovsky Institute of Virology, Gamaleya National Research Center of Epidemiology and Microbiology, Ministry of Health of the Russian Federation, Moscow 123098, Russia;3. Institute of Carcinogenesis, FSBI “N.N. Blokhin National Medical Research Center of Oncology”, The Ministry of Health of the Russian Federation, Kashirskoye Av., 24, Moscow, Russia |
| Abstract: | A series of DNA minor groove binding fluorescent dimeric bisbenzimidazoles DBA(n) bearing linkers of various length were synthesized and their biochemical and antiviral activities were evaluated. Their antiviral activity was assessed in model cell systems infected with human herpes simplex virus (HSV-1) and cytomegalovirus (CMV). Compounds DBA(1) and DBA(7) demonstrated in vitro inhibitory properties towards HSV-1, and DBA(7) completely blocked the viral infection. Compound DBA(11) displayed the in vitro therapeutic activity towards both HSV-1 and CMV. All of the DBA(n) could fluoresce, were well soluble in water, not cytotoxic to a concentration of 240?µM, penetrated well into cell nuclei by binding to DNA and could inhibit topo-I at low micromolecular concentrations. |
| Keywords: | topo-I DNA topoisomerase I DMT DNA methyltransferase HSV-1 herpes simplex virus type 1 CMV cytomegalovirus scDNA supercoiled DNA b.p. base pairs MABs monoclonal antibodies ACV acyclovir PBS phosphate buffered saline PFU/cells plaque formation units per cells cytotoxic dose TBTU BOP (benzotriazol-1-yloxy)tris(dimethylamino)-phosphonium hexafluorophosphate Phth-GlyOH NMM DIPEA Corresponding author. |
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