On the medicinal chemistry of gold complexes as anticancer drugs

Abstract: Metal complexes have shown interesting preclinical and clinical results as antitumor drugs and platinum compounds are well established in current cancer chemotherapy. However, the platinum based treatment of tumoral diseases is massively hampered by severe side effects and resistance development. Consequently, the development of novel metallodrugs with a pharmacological profile different from that of the platinum drugs is in the focus of modern medicinal chemistry and drug design. Among the non-platinum antitumor drugs, gold complexes have recently gained considerable attention due to their strong antiproliferative potency. In many cases the cell growth inhibiting effects could be related to anti-mitochondrial effects making gold species interesting drug candidates with a mode of action different from that of the platinum agents. The spectrum of gold complexes described as antiproliferative compounds comprises a broad variety of different species including many phosphine complexes as well as gold in different oxidation states. This presentation gives an overview of the relevant medicinal chemistry of known gold complexes with in vitro and in vivo tumor growth inhibiting properties. [Copyright &y& Elsevier]