DNA Sequence-Specific Ligands: XIV. Synthesis of Fluorescent Biologically Active Dimeric Bisbenzimidazoles DB(3,4,5,7,11)

被引:14
|
作者
Ivanov, A. A. [2 ]
Salyanov, V. I. [1 ]
Strel'tsov, S. A. [1 ]
Cherepanova, N. A. [3 ]
Gromova, E. S. [3 ]
Zhuze, A. L. [1 ]
机构
[1] Russian Acad Sci, VA Engelhardt Mol Biol Inst, Moscow 119991, Russia
[2] Russian Acad Med Sci, Blokhin Russian Oncol Res Ctr, Res Inst Carcinogenesis, Moscow 115478, Russia
[3] Moscow MV Lomonosov State Univ, Fac Chem, Moscow 119899, Russia
基金
俄罗斯基础研究基金会;
关键词
dimeric bisbenzimidazole; synthesis; fluorescence; CD; DNA; minor groove ligand; site-specificity; DNA topoisomerase I; inhibitor; DNA methyltransferase; MINOR-GROOVE; HOECHST-33258; MOLECULES; IN-VITRO; BINDING; METHYLTRANSFERASES; CANCER; INHIBITORS; ACIDS;
D O I
10.1134/S1068162011040054
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Five fluorescent symmetrical dimeric bisbenzimidazoles DB(n) containing four 2,6-substituted benzimidazole cores and differing in the length of the oligomethylene linker between two bisbenzimidazole rings (n = 3, 4, 5, 7, 11) have been synthesized. The ability of the dimeric bisbenzimidazoles to form complexes with the double-stranded DNA has been shown by spectral methods. Upon binding to the double-stranded DNA, DB(n) are localized in the narrow groove. The data on the inhibition of the DNA methyl-transferase Dnmt3a by DB(n) indicate that dimeric bisbenzimidazoles DB(3) and DB(11) site-specifically bind to the oligonucleotide duplex.
引用
收藏
页码:472 / 482
页数:11
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