Afive ceftriaxone antibiotic (ctx) complexes with Ca(II), Zn(II), Fe(III), Au(III) and Pd(II) metal ions were synthesized by 1:1 M ratio between of ceftriaxone hydrated sodium salt (Na2ctx) with CaCl2,ZnCl2, FeCl3.6H2O, AuCl3 and PdCl2metal salts in water–methanol medium. The complexes were well characterized dependent on the microanalytical (C,H, N), molar conductance, (FTIR, Raman, 1 HNMR and UV–Vis) spectroscopies, and magnetic measurements. The surface morphology and calculation of particle size of ceftriaxone complexes were performed based on SEM, TEM and X-ray diffraction. Calcium(II), zinc(II), and iron(III) complexes are six-coordinate with distorted octahedral geometry, while gold(III) and palladium(II) are four-coordination mode. The ceftriaxone drug acts as a tetradentate ligand towardsfive metal ions through N (amino group) and O (triazine,β-lactam carbonyl, and carboxylate groups) with the molecular formulas [Ca(ctx)(H2O)2].5H2O(1), [Zn(ctx)(H2O)2].7H2O (2), [Fe(ctx)(H2O)(Cl)].7H2O(3), [Au(ctx)].Cl. 4H2O(4) and [Pd(ctx)].3H2O(5). The cytotoxicity assays study of gold(III) complex against colon carcinoma cells (HCT-116) and hepatocellular carcinoma cells (HepG-2) showed that the 50% inhibitory concentration (IC50) of [Au(ctx)].Cl.4H2O against HepG-2 cell line is 8.53μg higher than that of HCT-116 cell line 20.5μg