Novel quinazolin-4-one derivatives as potentiating agents of doxorubicin cytotoxicity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F19%3A00536390" target="_blank" >RIV/60162694:G44__/19:00536390 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11150/19:10380868 RIV/00179906:_____/19:10380868
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S004520681830806X" target="_blank" >https://www.sciencedirect.com/science/article/pii/S004520681830806X</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bioorg.2018.10.001" target="_blank" >10.1016/j.bioorg.2018.10.001</a>
Alternative languages
Result language
angličtina
Original language name
Novel quinazolin-4-one derivatives as potentiating agents of doxorubicin cytotoxicity
Original language description
We report the design, synthesis and biological evaluation of 17 novel 8-aryl-2-morpholino-3,4-dihydroquinazoline derivatives based on the standard model of DNA-PK and PI3K inhibitors. Novel compounds are sub-divided into two series where the second series of five derivatives was designed to have a better solubility profile over the first one. A combination of in vitro and in silico techniques suggested a plausible synergistic effect with doxorubicin of the most potent compound 14d on cell proliferation via DNA-PK and poly(ADP-ribose) polymerase-1 (PARP-1) inhibition, while alone having a negligible effect on cell proliferation.
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
10608 - Biochemistry and molecular biology
Result continuities
Project
<a href="/en/project/TG02010020" target="_blank" >TG02010020: Centre for Transfer of Biomedical Technologies - PoC</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach<br>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
Bioorganic Chemistry
ISSN
0045-2068
e-ISSN
1090-2120
Volume of the periodical
82
Issue of the periodical within the volume
Feb
Country of publishing house
US - UNITED STATES
Number of pages
7
Pages from-to
204-210
UT code for WoS article
000455479600022
EID of the result in the Scopus database
2-s2.0-85054745766