In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
The result's identifiers
Result code in 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>
Alternative codes found
RIV/61989592:15310/19:73597240 RIV/00179906:_____/19:10393733
Result on the web
<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>
Alternative languages
Result language
angličtina
Original language name
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Original language description
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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN
1475-6366
e-ISSN
1475-6374
Volume of the periodical
34
Issue of the periodical within the volume
1
Country of publishing house
GB - UNITED KINGDOM
Number of pages
21
Pages from-to
877-897
UT code for WoS article
000462993400001
EID of the result in the Scopus database
2-s2.0-85063866757