Two novel copper (II) complexes [Cu(TFP)(Gly)Cl] • 2H 2 O complex (1) and [Cu(TFP)(His)Cl] • 2H 2 O complex (2) are synthesized, where TFP stands for trifluropromazine, Gly. represents glycine, and His. is histidine. Chemical composition, IR, mass spectra, and magnetic susceptibility tests are performed. Complex binding with macromolecules was investigated using UV-vis, viscosity, gel electrophoresis, and fluorescence quenching. Fluorescence spectroscopy revealed that each complex could replace ethidium bromide (EB). These complexes exhibit grooved, non-covalent, and electrostatic interactions with CT-DNA. Spectroscopy analysis of the BSA interaction showed that complexes bind to protein (K b values for (1) is 5.89 × 10 3 M À 1 and for (2) is 9.08 × 10 3 M À 1 ) more strongly than CT-DNA (K b values for (1) is 5.43 × 10 3 M À 1 and for (2) is 7.17 × 10 3 M À 1 ). Molecular docking analysis and spectral absorption measurements showed high agreement. Antimicrobial, antioxidant, and anti-inflammatory properties were tested in vitro. The druggability of complex (2) should be tested in vivo as it is more biologically active.