Abstract: This study comprised the preparation of Schiff base derivatives of cephalexin antibiotic by condensation reaction with Isatin. Metal complexes of the Schiff base ligands with Co(II), Ni(II), Cu(II), Cd(II) ions were prepared by reacting the ligand with the metal salts in refluxing ethanol. The chemical structure of the ligand, as well as the stereo-chemical structure and arrangements of the synthesized metal complexes were mentioned relying upon the outcomes given from TG analysis and CHN, mass, NMR, atomic absorption and FTIR, spectrophotometry, electronic spectra, measurements of conductivity and magnetic moments. The mole ratio of (ligand: metal ion) was (2:1) with bi-dentate linking demeanors of the chelating ligand with the metal ions. The IR spectra clarified a bidentate ligand which chalets through nitrogen atom of imino from azomethine bond and the oxygen atom of the carbonyl. UV-Vis spectrophotometry showed the characteristic absorption bands conformable to an octahedral arrangement for all metal complexes. The overall form found from empirical values was found to be M(OADC)₂(H2O)₂ where M = Co(II), Ni(II), Cu(II), Cd(II) and (OADC) = Schiff base ligand. This composition was further confirmed by thermal analysis and their thermal constancy in nitrogen atmosphere was carried out. The study of antibacterial appeared that the efficiency of metal complexes is higher than the one established for the free Schiff base ligand. Lastly, the cytotoxicity of [OADC] ligand and its complexes were screened on the cell line of Hep G2. [OADC] ligand appears good efficacy with the cell line of Hep G2 than complexes.