A series of platinum(II) complexes bearing N-heterocyclic carbene NHC of the type [(NHC)PtX(L)] where L is a dithiocarbamate ligand and X iodide were prepared and fully characterized. The molecular structure of one derivative was determined by single-crystal X-ray analyses confirming that the dithiocarbamate is acting as a bidentate ligand to the metal. All complexes demonstrated potent in vitro antiproliferative activities against cancer cells. Mechanistic investigations revealed that mitochondrial dysfunction and ROS (Reactive Oxygen Species) production were correlated with the cytotoxic process induced by these complexes.