The accidental discovery of cisplatin, cis-diaminodichloroplatinum (II), by Rosenberg and Van Camp in 1969, as a
chemotherapeutic agent opened a new perspective by including metal complexes as possible antitumor agents [1,2]. Cisplatin was
approved in the medical clinic, by Food and Drug Administration of the United States in 1978, and its importance in the treatment of
various types of cancer, such as testicular, ovarian and pulmonary carcinoma is unequivocal [3,4]. However, the use of cisplatin has
shown some limitations, such as the appearance of side effects, low solubility in water, and, especially, the development of cellular
resistance [5,6]. The limitations in the treatment of neoplasic diseases with cisplatin have encouraged diverse research groups in
the pursuit of other metal complexes, which should be more active and less toxic. An alternative would be replacing the metal center.
In this context, copper complexes have shown to be an interesting alternative. Copper is an essential metallic ion that is involved in
numerous biological process, playing an important role in diverse cellular function. In addition, copper may be less toxic for normal
cells rather than to cancer cells [7,8]. The anoxic characteristic of cancer cells promotes the reduction of Cu(II) to Cu(I), which is not
possible in normal cells. Cu(I) can catalyze the formation of reactive oxygen species (ROS) and induce lipidic peroxidation [9-11].