The use of anticancer agents forms an important part for treatment of cancer of various types. Complexes with cis-platinum compounds have been used for the prevention and treatment of cancers. Quite a number of these metalcontaining complexes have been isolated, chemically prepared and characterized for the treatment of cancer. Many of these compounds display potent cytotoxic effects, although there is a considerable progress made in the design of novel anticancer agents. Some of these compounds showed strong inhibitory effects on cancer growth with a potential to become anti-cancer drugs. However, the unwanted deleterious effects hamper the common use of these agents as anticancer drugs. Nevertheless, the use of protective agents during, before or after treatment with anti-cancer agents in combination therapy has proven effective in the treatment. The results prompt the study of the biologic activities and the design of better modality for treatment and prevention of cancer. Here, we review the potential and reduction of cytotoxic properties of the prominent member of this class of metal compounds for the treatment of cancer.