Characteristics of complex formation between monomeric and dimeric bisbenzimidazoles and AT-containing polynucleotide].

Double-stranded DNA is a one of the most important intracellular anticancer agent targets. Disturbance of DNA functions as well as DNA structure lead to disorder of such processes as transcription and/or translation thus inducing tumor cells death. Complex formation between novel dimeric bisbenzimidazole DB(7) and poly(dA-dT) duplex in comparison with known monomeric bisbenzimidazole MB(Ac) was investigated in this study. DB(7)-poly(dA-dT) binding constant was determined by fluorescence spectroscopy using Scatchard plot and it values 1.18 x 10(8) M(-1) that is two orders of magnitude larger than MB(Ac) one (2.06 x 10(6) M(-1)). Thus, from findings mentioned above it could be concluded that the presence of two bisbenzimidazole moieties in the ligand structure significantly increases its affinity to the polynucleotide which motivates the synthesis of new potential anticancer drugs based on dimeric bisbenzimidazoles.

Citation

E S Lisitsina, N A Durandin, A A Ivanov, S A Strel'tsov, O Iu Susova, A A Shtil', A L Zhuze, V A Kuz'min. Characteristics of complex formation between monomeric and dimeric bisbenzimidazoles and AT-containing polynucleotide]. Molekuliarnaia biologiia. 2012 Nov-Dec;46(6):922-7

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PMID: 23350239

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