Abstract
AbstractA 3‐formyl‐chromone‐appended zinc(II) intercalator drug candidate of the formulation [bis(chromone)(H 2 O)2 Zn(II)] was prepared as a potent anticancer agent and thoroughly characterized by multi‐spectroscopic and single X‐ray crystallographic studies. Preliminary binding studies of complex 1 with ct‐DNA/tRNA were carried out employing various complementary biophysical techniques and the corroborative results of these experiments suggested strong binding propensity via intercalation binding mode towards ct‐DNA/tRNA therapeutic targets, with higher preference for tRNA as quantified by binding constant { K b , K and K sv } parameters. The cleavage studies with pBR322 DNA were performed which implied that 1 cleaved the DNA by hydrolytic cleavage pathway which was further validated by T4 religation assay. Moreover, 1 was found to exhibit the tRNA cleavage behavior in a concentration and time‐dependent manner. The cytotoxicity of complex 1 was evaluated against Huh‐7, DU‐145 and the PNT2 cell lines by MTT assay. A dose‐dependent growth inhibition of the Huh‐7 and DU‐145 cells at low micromolar concentrations was observed and in another set of experiments, lipid peroxidation & glutathione (GSH) depletion were induced in the presence of the tested drug candidate. Interestingly, drug candidate 1 demonstrated selective cytotoxic activity for the DU‐145 cancer cell line with LC50 value of 3.2 μM which was further visualized by confocal microscopy.
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