This article presents the synthesis, structure characterization and biological affinity of the copper(II) complex with N-donor ligand, 2,2′-dipyridylamine (bipyam) results in the formation of [Cu(II)(bipyam)2Cl]. In this complex, dipyridylamine ligand coordinate to Cu(II) atom in a bidentate mode with two pyridine nitrogen atoms. The molecular structure of the complex reveals a regular trigonal-based pyramidal geometry. This complex interacts with human (HSA) and bovine serum (BSA) albumin proteins have been studied by fluorescence spectroscopy technique and the obtained results reveal an excellent binding propensity in both cases in comparison to the ligand (Kb = 7.6 × 105, M−1 in BSA and Kb = 1.64 × 105, M−1 in HSA). UV spectroscopy titrations shows that the [Cu(bipyam)2Cl] interact with DNA through intercalation mode with comparatively high binding constant value (Kb) = 4.18 × 104, M−1. Complex interact with DNA was also studies by gel electrophoresis, circular dichroism and fluorescence spectroscopy methods. The fluorescence titration experiment is based on the decreasing of the emission intensity which show the replacement of EtBr from DNA bound EtBr solution, showing that complex bind to DNA via intercalative mode in strong competition to EtBr. The copper(II) complex show potential cytotoxicity against human breast cancer cell lines (MCF-7).