A series of complexes containing titanium, Ti, as a metal center has shown to possess a wide spectrum of antitumor properties. This series belongs to the non-platinum metal antitumor agents which has been developed mainly in the past 20 years. The bis(beta-diketonato)titanium(IV) and titanocene derivatives appear to offer a different alternative for cancer chemotherapy which do not follow the rationale and mechanism of action of the platinum complexes. The hydrolysis of these complexes in aqueous and pseudo aqueous solutions is discussed and the interaction studies of titanium complexes with biomolecules are also presented to unravel the mechanism of action at molecular levels.