Tacrine derivatives as dual topoisomerase I and II catalytic inhibitors

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F15%3A00446307" target="_blank" >RIV/68081707:_____/15:00446307 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00179906:_____/15:10293865

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.bioorg.2015.03.002" target="_blank" >http://dx.doi.org/10.1016/j.bioorg.2015.03.002</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bioorg.2015.03.002" target="_blank" >10.1016/j.bioorg.2015.03.002</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Tacrine derivatives as dual topoisomerase I and II catalytic inhibitors

Popis výsledku v původním jazyce

This study examines the binding properties of a series of newly synthetized tacrine derivatives 1-4 and their anticancer effects. Spectroscopic techniques (UV-Vis, fluorescence spectroscopy, thermal denaturation, and linear spectropolarimetry) and viscometry were used to study DNA binding properties and to determine the types of DNA interaction with the studied derivatives. The binding constants for the complexes with DNA were obtained using UV-Vis spectroscopic titrations (K = 1.6 x 10(4)-4.0 x 10(5) M-1) and electrophoretic methods were used to determine the effect of the derivatives on topoisomerase I and II activity. Monotacrine derivative 1 showed evidence of topoisomerase I relaxation activity at a concentration of 30 x 10(-6) M, while bistacrinederivatives 2-4 produced a complete inhibition of topoisomerase I at a concentration of 5 x 10(-6) M. The biological activities of the derivatives were studied using MTT-assay and flow cytometric methods (detection of mitochondrial membr

Název v anglickém jazyce

Tacrine derivatives as dual topoisomerase I and II catalytic inhibitors

Popis výsledku anglicky

This study examines the binding properties of a series of newly synthetized tacrine derivatives 1-4 and their anticancer effects. Spectroscopic techniques (UV-Vis, fluorescence spectroscopy, thermal denaturation, and linear spectropolarimetry) and viscometry were used to study DNA binding properties and to determine the types of DNA interaction with the studied derivatives. The binding constants for the complexes with DNA were obtained using UV-Vis spectroscopic titrations (K = 1.6 x 10(4)-4.0 x 10(5) M-1) and electrophoretic methods were used to determine the effect of the derivatives on topoisomerase I and II activity. Monotacrine derivative 1 showed evidence of topoisomerase I relaxation activity at a concentration of 30 x 10(-6) M, while bistacrinederivatives 2-4 produced a complete inhibition of topoisomerase I at a concentration of 5 x 10(-6) M. The biological activities of the derivatives were studied using MTT-assay and flow cytometric methods (detection of mitochondrial membr

Druh

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

CEP obor

BO - Biofyzika

OECD FORD obor

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Projekt

<a href="/cs/project/LD14019" target="_blank" >LD14019: Molekulární a buněčná farmakologie nových konjugovaných organokovových sloučenin. Vztah k vývoji nových léčiv proti rakovině.</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

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

59

Číslo periodika v rámci svazku

APR2015

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

9

Strana od-do

168-176

Kód UT WoS článku

000352211900016

EID výsledku v databázi Scopus

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