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The reaction of the newly synthesized ligand, 2-isonicotinoyl-Nphenylhydrazine-1-carbothioamide (H 3 L), with acetate salt of Co (II), Cu (II), Ni (II) and Zn (II) led to isolation of four solid complexes. The ligand and complexes structure elucidation were based on elemental analyses, spectral analyses (IR, UV-Visible, 1 H and 13 C-NMR, MS and ESR), TGA, molar conductivity and magnetic moments measurements. The results indicated that the ligand exists in the thioketo form, while on coordination to the metal ions; it behaves as mono-negative bidentate chelate and exists in enol form. The optical band gap measurements of the ligand and its metal complexes are in the range 3.83-4.48 eV indicating their semi-conducting character. The cytotoxicity examination of H 3 L and its Zn (II) complex showed that the ligand have very strong cytotoxicity against both HCT-116 and HEPG-2 cell lines while, Zn (II) complex has moderate activity.