Number of the records: 1  

Novel trisubstituted acridines as human telomeric quadruplex binding ligands

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    SYSNO ASEP0439913
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleNovel 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, ORCID
    Number of authors18
    Source TitleBioorganic Chemistry. - : Elsevier - ISSN 0045-2068
    Roč. 57, DEC 2014 (2014), s. 13-29
    Number of pages17 s.
    Publication formPrint - P
    Languageeng - English
    CountryUS - United States
    KeywordsBraco 19 derivatives ; Trisubstituted acridines ; DNA binding
    Subject RIVBO - Biophysics
    Institutional supportBFU-R - RVO:68081707
    UT WOS000345698000003
    DOI https://doi.org/10.1016/j.bioorg.2014.07.010
    AnnotationA 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.
    WorkplaceInstitute of Biophysics
    ContactJana Poláková, polakova@ibp.cz, Tel.: 541 517 244
    Year of Publishing2015
Number of the records: 1  

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