Novel trisubstituted acridines as human telomeric quadruplex binding ligands

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F14%3A00439913" target="_blank" >RIV/68081707:_____/14:00439913 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.bioorg.2014.07.010" target="_blank" >http://dx.doi.org/10.1016/j.bioorg.2014.07.010</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bioorg.2014.07.010" target="_blank" >10.1016/j.bioorg.2014.07.010</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Novel trisubstituted acridines as human telomeric quadruplex binding ligands

Popis výsledku v původním jazyce

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 primarytrend 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 d

Název v anglickém jazyce

Novel trisubstituted acridines as human telomeric quadruplex binding ligands

Popis výsledku anglicky

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 primarytrend 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 d

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

BO - Biofyzika

OECD FORD obor

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Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Bioorganic Chemistry

ISSN

0045-2068

e-ISSN

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Svazek periodika

57

Číslo periodika v rámci svazku

DEC 2014

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

17

Strana od-do

13-29

Kód UT WoS článku

000345698000003

EID výsledku v databázi Scopus

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