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Tytuł: Design, synthesis and in Vitro activity of anticancer styrylquinolines. The p53 Independent Mechanism of Action
Autor: Mrozek-Wilczkiewicz, Anna
Spaczyńska, Ewelina
Malarz, Katarzyna
Cieślik, Wioleta
Rams-Baron, Marzena
Musioł, Robert
Słowa kluczowe: styrylquinoline; styrylquinoline derivative; protein p53; antineoplastic agent; colon carcinoma cell; TP53 gene
Data wydania: 2015
Źródło: PLoS ONE, iss. 11 (2015), art. no e0142678
Abstrakt: A group of styrylquinolines were synthesized and tested for their anti-proliferative activity. Anti-proliferative activity was evaluated against the human colon carcinoma cell lines that had a normal expression of the p53 protein (HCT116 p53+/+) and mutants with a disabled TP53 gene (HCT116 p53-/-) and against the GM 07492 normal human fibroblast cell line. A SAR study revealed the importance of Cl and OH as substituents in the styryl moiety. Several of the compounds that were tested were found to have a marked anti-proliferative activity that was similar to or better than doxorubicin and were more active against the p53 null than the wild type cells. The cellular localization tests and caspase activity assays suggest a mechanism of action through the mitochondrial pathway of apoptosis in a p53-independent manner. The activity of the styrylquinoline compounds may be associated with their DNA intercalating ability.
DOI: 10.1371/journal.pone.0142678
ISSN: 1932-6203
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