The present study aims at synthesizing three new copper(ii) complexes of maltol in the presence of 1,10-phenanthroline-, 2,2 '-bipyridine- and 4,4-dibromo-2,2 '-bipyridine ligands. The structure of the Cu(ii) complexes was characterized by FTIR, CHN analysis and X-ray crystallography. The interaction of the Cu(ii) complexes with human serum albumin (HSA) was studied using various methods including fluorescence spectroscopy, UV-visible spectroscopy and molecular docking. The cytotoxic activity of the complexes was investigated using human breast cancer cells (MCF-7), and the results were compared with the activity of cis-platin as a positive control. The data showed that the complex 1, [Cu(mal)(4,4-dibromo-2,2 '-bpy)(H2O)]center dot NO3, has the highest cytotoxicity among the compounds. The experiment indicated that the quenching process of HSA fluorescence by complexes 1-4 and the maltol ligand is a static mechanism. In addition, the results provided information about thermodynamic parameters and the number of binding sites. The high values of K-b show that the complexes can bind strongly with HSA. The results from the UV-Visible spectroscopy studies demonstrated that conformational alterations occurred in the secondary structure of HSA due to binding with the complexes.