Synthesis, structural characterization and antiproliferative activity on MCF-7 and A549 tumor cell lines of [Cu(N-N)(β3-aminoacidate)]NO3 complexes (Casiopeínas®)

The synthesis and complete characterization of three new mixed chelate copper (II) complexes {[Cu(1,10-phenathroline)(β-aminoacidate)]NO3·x(solv)} is reported. In vitro studies revealed that complexes have growth inhibition activity against MCF-7 and A549 tumor cell lines. The experimental E1/2 values for the complexes could be correlated with their anticancer activities. [Display omitted] •The synthesis of three new mixed chelate copper (II) complexes containing β3-aminoacidates.•In vitro studies on MCF-7 and A549 tumor cell lines.•Full physical, physicochemical, and spectroscopic characterizations.•Correlation between the E1/2 values and IC50 values.•Structural analysis of the three new complexes through single crystals X-ray diffraction analysis. The synthesis of three new mixed chelate copper (II) nitrate coordination compounds of the general formula {[Cu(phen)(L)(solv)]NO3· 0–0.5(solv)} is reported, where phen is 1,10-phenanthroline and L is a β3-aminoacidate (β-alaninate for 1, 3-aminobutanoate for 2 and 3-amino-3-cyclohexylpropanoate for 3), and the solvent (solv) is H2O and/or MeOH. The complexes were characterized by elemental analysis, IR and UV–Vis spectrophotometry, EPR spectroscopy, effective magnetic moment, conductometric and cyclovoltammetric measurements as well as single-crystal X-ray diffraction (SCXRD) analysis. All complexes are mononuclear Cu(II) complexes with d9 configuration. In solution, the compounds are 1:1 electrolytes and exhibit square-based pyramidal coordination polyhedra. Meanwhile, in the solid state the coordination geometries are square-based pyramidal for compounds 1 and 2, but distorted octahedral for compound 3 due to coordination of the nitrate counterion. In vitro studies revealed that compounds 1, 2 and 3 have growth inhibition activity against MCF-7 and A549 tumor cell lines. The clustering of the experimental half-wave potential values among the three complexes could be explained by the fact of that the substitution pattern was changed on the secondary ligand, while the primary ligand remains without any structural modification.