This work presents a multifaceted mechanism of the anticancer action of a 2-styrylquinazoline derivative. Extensive analysis of various aspects related to tyrosine kinase inhibition and effects on cellular targets at both the gene and protein levels revealed the potential of this IS20 compound for future research. This study presents a detailed analysis of the relationship between ABL and SRC kinase affecting the inhibition of the EGFR/mTOR signaling pathway in a non-obvious manner. The study was supported by experiments using various molecular biology techniques to confirm the induction of oxidative stress, inhibition of the cell cycle in the G2/M phase and the triggering of cell death via both the apoptosis and autophagy pathways. The cell models included those with different p53 protein status, which affected the cellular response in the form of altered Ndrg1 expression. Finally, the appropriate physicochemical properties of IS20 for adequate bioavailability and toxicity to the body were observed in an in vivo model.

• Klíčová slova
• Ndrg1, Anticancer drug, Apoptosis, Autophagy, Iron chelator, Oxidative stress, Styrylquinazoline, p53 protein,
• MeSH
• apoptóza účinky léků   MeSH
• autofagie účinky léků   MeSH
• chinazoliny * farmakologie   chemie   MeSH
• erbB receptory metabolismus   MeSH
• intracelulární signální peptidy a proteiny * genetika   metabolismus   MeSH
• lidé MeSH
• myši MeSH
• nádorové buněčné linie MeSH
• nádorový supresorový protein p53 metabolismus   MeSH
• oxidační stres * účinky léků   MeSH
• proteiny buněčného cyklu * genetika   metabolismus   MeSH
• protinádorové látky * farmakologie   chemie   MeSH
• signální transdukce účinky léků   MeSH
• TOR serin-threoninkinasy metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• chinazoliny * MeSH
• erbB receptory MeSH
• intracelulární signální peptidy a proteiny * MeSH
• N-myc downstream-regulated gene 1 protein MeSH Prohlížeč
• nádorový supresorový protein p53 MeSH
• proteiny buněčného cyklu * MeSH
• protinádorové látky * MeSH
• TOR serin-threoninkinasy MeSH