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.

A Chełkowski Institute of Physics University of Silesia Katowice Poland

Institute of Chemistry University of Silesia Katowice Poland

Laboratory of Growth Regulators Centre of the Region Haná for Biotechnological and Agricultural Research Palacký University and Institute of Experimental Botany AS CR Olomouc Czech Republic

Silesian Center for Education and Interdisciplinary Research University of Silesia Chorzów Poland

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Chemistry towards Biology-Instruct: Snapshot

Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action

The Forty-Sixth Euro Congress on Drug Synthesis and Analysis: Snapshot †

The Eighth Central European Conference "Chemistry towards Biology": Snapshot