Metal complexes play an essential role in chemical and medicalsciences for their importance and variety of actions. Schiff bases were multifunctional pharmacophores able to form chelating complexes with several metals in different oxidation states. Complexes with Schiff bases are widely described in the literature for their multiple actions and numerous advantages, such as low cost and easy synthesis. They show multifunctional bio-activities, such as antimicrobial, antioxidant, antimalarial, anti-inflammatory and antitumor, anticancer, DNA binding etc. Schiff bases may also form complexes with many Inner-transition elements acting as catalysts (e.g., in various synthetic processes) and antitumor agents. This review offers to extends preparation and the uses of Schiff bases as antitumorals, highlighting the importance, in the field of the anticancer agents, of these tools as ligands of metal complexes.