Four novel copper(II) complexes of 2‐aminobenzimidazole derivatives (obtained from the Knoevenagel condensation of acetylacetone (obtained from acetylacetone and halogen‐substituted benzaldehydes) and 2‐aminobenzimidazole) were synthesized. They were characterized using elemental analysis, molar conductance measurements, and fast atom bombardment mass, Fourier transform infrared, NMR, UV–visible and electron paramagnetic resonance spectroscopies. On the basis of the spectral studies, a distorted square planar geometry was assigned for all the complexes. The antibacterial screening of the ligands and their complexes revealed that all the complexes had higher activities than the free ligands. Superoxide dismutase and antioxidant activities of the copper complexes were also studied. The shifts in ΔEp, E1/2, Ipc and Ipa values were explored for the interaction of the complexes with calf thymus DNA using the electrochemical technique.

5-carbethoxy-2-thiouracil (eitotH2) reacts with CuX (X= Cl, Br, I) halides to give the formula [CuX(eitotH)2]2 dinuclear complexes, while the formula [CuX(PPh3)2(eitotH)2] mononuclear mixed ligand complexes result when reaction is carried out in the presence of two equivalent of triphenylphosphine (PPh3). The new copper (I) complexes were studied against two tumor cell lines, A549 (human pulmonary carcinoma cell line) and HeLa (human epithelial carcinoma cell line) and one regular immortalized cell line, MRC5 (human fetal lung fibroblast). In comparison to the phosphine free ones that hindered cell proliferation only at relatively high concentration, the mixed ligand complexes with triphenylphosphine were found to be extremely cytotoxic. Keywords: Copper (I), 5-carbethoxy-2-thiouracil (eitotH2), Triphenylphosphine, in vitro cytotoxicity, carcinoma cell lines

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