1. DNA specific fluorescent symmetric dimeric bisbenzimidazoles DBP(n): the synthesis, spectral properties, and biological activity.
- Author
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Ivanov AA, Koval VS, Susova OY, Salyanov VI, Oleinikov VA, Stomakhin AA, Shalginskikh NA, Kvasha MA, Kirsanova OV, Gromova ES, and Zhuze AL
- Subjects
- Animals, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Bisbenzimidazole chemical synthesis, Bisbenzimidazole pharmacology, Cell Line, DNA genetics, DNA-Cytosine Methylases antagonists & inhibitors, Dimerization, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Fluorescent Dyes chemistry, Gene Expression drug effects, Humans, MCF-7 Cells, Mice, Microscopy, Fluorescence, Structure-Activity Relationship, Topoisomerase I Inhibitors chemical synthesis, Topoisomerase I Inhibitors chemistry, Topoisomerase I Inhibitors pharmacology, Bisbenzimidazole analogs & derivatives, DNA chemistry, DNA drug effects, Fluorescent Dyes chemical synthesis, Fluorescent Dyes pharmacology
- Abstract
A series of new fluorescent symmetric dimeric bisbenzimidazoles DBP(n) bearing bisbenzimidazole fragments joined by oligomethylene linkers with a central 1,4-piperazine residue were synthesized. The complex formation of DBP(n) in the DNA minor groove was demonstrated. The DBP(n) at micromolar concentrations inhibit in vitro eukaryotic DNA topoisomerase I and prokaryotic DNA methyltransferase (MTase) M.SssI. The DBP(n) were soluble well in aqueous solutions and could penetrate cell and nuclear membranes and stain DNA in live cells. The DBP(n) displayed a moderate effect on the reactivation of gene expression., (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Published
- 2015
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