Metals contribute important roles in biological system. It is recognized that metals are highly linked in cellular and subcellular functions. With the application of novel and experienced tools to study biological and biochemical systems the true role of inorganic salts in biological systems can be studied. Schiff base metal complexes show a broad range of biological activity. The activity of Schiff base ligand is usually increased by complexation with the metal ion. The copper complexes of Schiff bases have striking properties such as antibacterial, antifungal, antiviral, anti-inflammatory, anti-tumor and cytotoxic activities, plant development controller, enzymatic activity and applications in pharmaceutical fields. The divalent cations Zn 2+, Ca 2+ and Mg 2+ prevent cytotoxicity and in vivo antagonize Cd-induced carcinogenesis. Lack of body iron is common in cancer patients and it is associated with complications in surgery and in animal experiments. The transport of iron and other metal ions by the blood plasma is achieved through the formation of protein complexes. Copper is placed as a vital metalloelement and is primarily connected with copper-dependent cellular enzymes. Metals are also used as inorganic drugs for many diseases. In this review our main focused on research undertaken for biological activity study of Cu(II) metal complexes containing Schiff bases over the past few decades.