In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F19%3A00536660" target="_blank" >RIV/60162694:G44__/19:00536660 - isvavai.cz</a>
Nalezeny alternativní kódy
RIV/61989592:15310/19:73597240 RIV/00179906:_____/19:10393733
Výsledek na webu
<a href="https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1593159" target="_blank" >https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1593159</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1080/14756366.2019.1593159" target="_blank" >10.1080/14756366.2019.1593159</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Popis výsledku v původním jazyce
A combination of biochemical, biophysical and biological techniques was used to study calf thymus DNA interaction with newly synthesized 7-MEOTA-tacrine thiourea 12-17 and urea heterodimers 18-22, and to measure interference with type I and II topoisomerases. Their biological profile was also inspected in vitro on the HL-60 cell line using different flow cytometric techniques (cell cycle distribution, detection of mitochondrial membrane potential dissipation, and analysis of metabolic activity/viability). The compounds exhibited a profound inhibitory effect on topoisomerase activity (e.g. compound 22 inhibited type I topoisomerase at 1 mu M concentration). The treatment of HL-60 cells with the studied compounds showed inhibition of cell growth especially with hybrids containing thiourea (14-17) and urea moieties (21 and 22). Moreover, treatment of human dermal fibroblasts with the studied compounds did not indicate significant cytotoxicity. The observed results suggest beneficial selectivity of the heterodimers as potential drugs to target cancer cells.
Název v anglickém jazyce
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Popis výsledku anglicky
A combination of biochemical, biophysical and biological techniques was used to study calf thymus DNA interaction with newly synthesized 7-MEOTA-tacrine thiourea 12-17 and urea heterodimers 18-22, and to measure interference with type I and II topoisomerases. Their biological profile was also inspected in vitro on the HL-60 cell line using different flow cytometric techniques (cell cycle distribution, detection of mitochondrial membrane potential dissipation, and analysis of metabolic activity/viability). The compounds exhibited a profound inhibitory effect on topoisomerase activity (e.g. compound 22 inhibited type I topoisomerase at 1 mu M concentration). The treatment of HL-60 cells with the studied compounds showed inhibition of cell growth especially with hybrids containing thiourea (14-17) and urea moieties (21 and 22). Moreover, treatment of human dermal fibroblasts with the studied compounds did not indicate significant cytotoxicity. The observed results suggest beneficial selectivity of the heterodimers as potential drugs to target cancer cells.
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
30107 - Medicinal chemistry
Návaznosti výsledku
Projekt
—
Návaznosti
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2019
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN
1475-6366
e-ISSN
1475-6374
Svazek periodika
34
Číslo periodika v rámci svazku
1
Stát vydavatele periodika
GB - Spojené království Velké Británie a Severního Irska
Počet stran výsledku
21
Strana od-do
877-897
Kód UT WoS článku
000462993400001
EID výsledku v databázi Scopus
2-s2.0-85063866757