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The synthesis, physicochemical characterizations, and biological investigations on the chelation of the antibiotic medication enoxacin (EXN) with certain vital metal ions, such as platinum(IV), ruthenium(III), and iridium(III) are discussed in this study. These compounds structures were interpreted based on elemental analysis and spectral measurements (FTIR, 1H-NMR, UV-Vis electronic, and XRD). The findings show that there is same coordination pathway for the chelation behavior of enoxacin complexes: a monodentate manner. The Pt(IV), Ru(III), and Ir(III) complexes are coordinated through the N atom of the piperazine ring, which is an unusual mode of coordination for this class of compounds. The dissolved complexes in DMSO were found to have non-electrolyte nature based on their molar conductance measurements. The formula for these complexes is [Pt(EXN)3(H2O)2Cl] (1), [Ru(EXN)3(H2O)3] (2), and [Ir(EXN)3(H2O)3] (3). Using scanning electron microscope (SEM) analysis and Xray powder diffraction (XRD), the nano-scale range of the Pt(IV), Ru(III), and Ir(III) complexes has been determined. Results of in vitro cytotoxicity were examined using MCF-7 cells (human breast cancer cell line) and HepG-2 cells (human hepatocellular carcinoma) that had been grown. The cytotoxic activity of the metal complexes demonstrated a cytotoxic effect against the growth of human breast and liver cancer cell lines. [ABSTRACT FROM AUTHOR]