Abstract
In this study, some new quinoline-carboxamide derivatives possessing a flexible (dimethylamino) ethylcarboxamide side chain were synthesized as DNA intercalating agents. Synthesized compounds displayed potent cytotoxic activities against three human cancer cell lines including colorectal adenocarcinoma cancer cells (HT-29), breast cancer cells (MCF-7) and lung cancer cells (A549). Compound 3d showed promisingantiproliferative activity (IC50= 3.97 to 6.67 µM) against cancer cells. The simplest compound (compound 3a) without substitution displayed the weakest cytotoxic effects ranging from 24.6 to 42.3 μM. The interaction of the most cytotoxic compound 3d with calf thymus DNA (ctDNA) was evaluated by fluorescence, UV absorption, resonance light scattering (RLS), melting studies, viscosity measurements, circular dichroism (CD) spectroscopy, molecular docking and molecular dynamic (MD). Generally, studies displayed a combined quenching via intercalating binding mode of compound 3d to ctDNA.
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