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Novel quinazolin-4-one derivatives as potentiating agents of doxorubicin cytotoxicity
M. Pospisilova, M. Andrs, M. Seifrtova, R. Havelek, D. Jun, P. Tomsik, L. Prchal, R. Dolezal, A. Tichy, T. Kucera, J. Korabecny, M. Rezacova,
Bioorganic chemistry.
2019 ;
82 (-) :
204-210.
[pub] 20181006
Language English Country United States
Document type Journal Article, Research Support, Non-U.S. Gov't
Persistent link
https://www.medvik.cz/link/bmc19034963
- MeSH
- Apoptosis drug effects MeSH
- HT29 Cells MeSH
- Quinazolinones chemical synthesis pharmacology toxicity MeSH
- Doxorubicin pharmacology MeSH
- Enzyme Inhibitors chemical synthesis pharmacology toxicity MeSH
- Nuclear Proteins antagonists & inhibitors MeSH
- Humans MeSH
- Morpholines chemical synthesis pharmacology toxicity MeSH
- Mice MeSH
- Animals, Outbred Strains MeSH
- Poly (ADP-Ribose) Polymerase-1 antagonists & inhibitors MeSH
- Cell Proliferation drug effects MeSH
- DNA-Activated Protein Kinase antagonists & inhibitors MeSH
- Antineoplastic Agents pharmacology MeSH
- Drug Design MeSH
- Drug Synergism MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Female MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
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.
References provided by Crossref.org
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