Recent studies of new metal complexes for antitumor properties have focused on the speeding up of the treatment process in chemotherapy. In this study, focus was put on the two new metal complexes, copper (LCu(OAc)2) and iron {LFeCl2[FeCl4]}complexes that have been synthesized. Both new complexes have been characterized by FT-IR and UV-Vis. In addition, the structures of two complexes have been established by the X-ray crystallography. The molecular structures of (LCu(OAc)2) and LFeCl2[FeCl4] have been determined confirming that the ligand is bidentate (N,N) imidazopyridine and adopted octahedral configurations. The two complexes and ligand L have been tested for biological activity against prostate cancer cell line LNCaP. The complexes have shown promising results for the anti-proliferative activity. Although the ligand displayed high cytotoxicity toward prostate cancer cell line, the complexes have shown far better cytotoxicity property than the ligand.