Počet záznamů: 1  

Novel trisubstituted acridines as human telomeric quadruplex binding ligands

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    0439913 - BFÚ 2015 RIV US eng J - Článek v odborném periodiku
    Ungvarsky, J. - Plšíková, J. - Janovec, J. - Koval, J. - Mikeš, J. - Mikesová, L. - Harvanova, D. - Fedoročko, P. - Kristian, P. - Kašpárková, Jana - Brabec, Viktor … celkem 18 autorů
    Novel trisubstituted acridines as human telomeric quadruplex binding ligands.
    Bioorganic Chemistry. Roč. 57, DEC 2014 (2014), s. 13-29. ISSN 0045-2068. E-ISSN 1090-2120
    Institucionální podpora: RVO:68081707
    Klíčová slova: Braco 19 derivatives * Trisubstituted acridines * DNA binding
    Kód oboru RIV: BO - Biofyzika
    Impakt faktor: 2.152, rok: 2014

    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.
    Trvalý link: http://hdl.handle.net/11104/0243098

     
     
Počet záznamů: 1  

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