In this study, a biologically active nickel(II) complex, [Ni(bipy)3]Cl2 (where bipy = 2,2′-bipyridine), was synthesized using a straightforward precipitation method. This nickel(II) complex was subsequently grafted onto anatase (TiO2) nanoparticles (NPs) through an adsorption technique, yielding nickel(II)-complex-grafted anatase (Ni-TiO2) NPs. The Ni-TiO2 NPs were thoroughly characterized using a range of analytical methods, including X-ray diffraction (XRD), Fourier-transform infrared (FT-IR) spectroscopy, UV–visible spectroscopy, scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDAX), which confirmed the successful grafting of the complex onto the TiO2 NPs and maintained the structural integrity of the composite. The anticancer activity of the Ni-TiO2 NPs was assessed on Non-Small Cell Lung Cancer (NSCLC) cell lines using the MTT assay, revealing a significant enhancement in anticancer efficacy, with a 69 % improvement in cell inhibition compared to untreated cells. Moreover, the antioxidant potential of the Ni-TiO2 NPs was evaluated using the 1-Diphenyl-2-picrylhydrazyl (DPPH) assay, and their anti-inflammatory activity was determined through the protein denaturation assay. Both assays demonstrated that the Ni-TiO2 NPs exhibited superior inhibitory effects compared to the precursor Ni(II) complex, indicating enhanced bioactivity.