The influence of cimetidine on patients under cisplatin treatment for cancer is controversial. It has moderate or no effects on several types of cancer and its effects on the nephrotoxicity induced by cisplatin are uncertain. To examine the binding properties and antiproliferative effects of the known anticancer noble metals, cimetidine (cim) was complexed to platinum(II) and palladium(II). The crystal structure of the Pt–cim compound shows two molecules of cimetidine coordinated to the metal through thioether sulfur and imidazolic nitrogen whereas spectroscopic studies in solution for Pd–cim reveal that the ratio of the metal to cimetidine is 1:1 with identical coordination environments. To determine the antitumor activity of the drugs, the interaction of the metallic complexes and free cimetidine with DNA was assessed. Their cytotoxic activity was compared with that of cisplatin.