Crystal structure and cytotoxic activity of Cu(ii) complexes with bis-benzoxazolylhydrazone of 2,6-diacetylpyridine

Based on bis-hetarylhydrazone H2L, a condensation product of 2,6-diacetylpyridine with 2-hydrazinobenzoxazole, a series of mononuclear copper(ii) coordination compounds have been synthesized: [Cu(HL)NO3], [Cu(HL)(H2O)]ClO4, [Cu(HL)X] (X = Br-, X = Cl-). The structure of the compounds has been studied by means of NMR, IR, ESR, X-ray absorption spectroscopy and X-ray single crystal diffraction methods. In the compounds the copper center is in the square pyramidal environment. All compounds have been screened in vitro for their cytotoxic activity against HepG2 and MRC-5 cell lines. The ligand H2L shows no cytotoxicity at tested concentrations (1-100 & mu;M), while all the Cu(ii) complexes exhibit significant dose-dependent cytotoxic effects with IC50 values in the range of 1.4-3.0 & mu;M (HepG2 cells).

Automated summary

Based on the bis-hetarylhydrazone H2L, a series of mononuclear copper(ii) coordination compounds were synthesized and their structures were studied using several methods. The copper center in these compounds is in a square pyramidal environment. The cytotoxic activity of the compounds against HepG2 and MRC-5 cell lines was evaluated, and the Cu(ii) complexes showed significant dose-dependent cytotoxic effects.