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Novel trisubstituted acridines as human telomeric quadruplex binding ligands
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SYSNO ASEP 0439913 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Novel trisubstituted acridines as human telomeric quadruplex binding ligands Author(s) Ungvarsky, J. (SK)
Plšíková, J. (SK)
Janovec, J. (SK)
Koval, J. (SK)
Mikeš, J. (SK)
Mikesová, L. (SK)
Harvanova, D. (SK)
Fedoročko, P. (SK)
Kristian, P. (SK)
Kašpárková, Jana (BFU-R) RID, ORCID
Brabec, Viktor (BFU-R) RID, ORCIDNumber of authors 18 Source Title Bioorganic Chemistry. - : Elsevier - ISSN 0045-2068
Roč. 57, DEC 2014 (2014), s. 13-29Number of pages 17 s. Publication form Print - P Language eng - English Country US - United States Keywords Braco 19 derivatives ; Trisubstituted acridines ; DNA binding Subject RIV BO - Biophysics Institutional support BFU-R - RVO:68081707 UT WOS 000345698000003 DOI https://doi.org/10.1016/j.bioorg.2014.07.010 Annotation A novel series of trisubstituted acridines were synthesized with the aim of mimicking the effects of BRACO-19. These compounds were synthesized by modifying the molecular structure of BRACO19 at positions 3 and 6 with heteroacyclic moieties. All of the derivatives presented in the study exhibited stabilizing effects on the human telomeric DNA quadruplex. UV-vis spectroscopy, circular dichroism, linear dichroism and viscosimetry were used in order to study the nature of the DNA binding in more detail. The results show that all of the novel derivatives were able to fold the single-stranded DNA sequences into antiparallel G-quadruplex structures, with derivative 15 exhibiting the highest stabilizing capability. Cell cycle analysis revealed that a primary trend of the "braco"-like derivatives was to arrest the cells in the Sand G(2)M-phases of the cell cycle within the first 72 h, with derivative 13 and BRACO19 proving particularly effective in suppressing cell proliferation. All studies derivatives were less toxic to human fibroblast cell line in comparison with HT 29 cancer cell line. (C) 2014 Elsevier Inc. All rights reserved. Workplace Institute of Biophysics Contact Jana Poláková, polakova@ibp.cz, Tel.: 541 517 244 Year of Publishing 2015
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