Square planar copper(II) complexes containing 7-methyl-2-oxo-1,2-dihydroquinoline-3-carboxaldehyde thiosemicarbazones were synthesized and structurally characterized by using various spectro-analytical techniques. Single crystal X-ray diffraction analysis of complexes P1 and P3 confirmed the mode of attachment of ligands. The binding affinity of the ligands and complexes with nucleic acid and albumin were studied by taking CT-DNA and BSA as models. The new complexes were subjected to screen their in vivo cytotoxic potential by taking C. elegans as suitable choice due to their sequenced genome and easy mutation production. Exposure of the complexes P1-P4 to the worms, up to 75 μM concentration it was found that there were no adverse effect in the physiological functions. Furthermore, the reduction in the tumor growth was confirmed by the DAPI/AO staining and the lifespan of gld-1 mutant strain JK1466 has been increased significantly with a mean survival increase of 66.4%. The stress tolerance or longevity was directly related to the anti-oxidant enzymes which can be quantified by GFP reporter strains. Under oxidative stress, as compared with the control, the relative mean fluorescence intensity of mutant worms was increased around 70–72% and 60–64% in sod-3 and hsp-16.2 expressions respectively. Interestingly, all the complexes P1-P4 have shown their potent effect on cytotoxic properties, physiological changes and also reduction in the tumor growth and there were no significant differences in their activity were found. Altogether, the research findings recommended that the candidature of the complexes P1-P4 to use as anti-tumor drugs based on further explorations.
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