This presentation will focus on research carried out in our labs. on organometallic compds. based on the ruthenium(II)-arene unit that exhibit promising in vitro and in vivo anticancer activity and potentially overcome the limitations of platinum based anticancer drugs. Recently we showed that our ruthenium(II)-arene compds. are able to selectively induce apoptosis in cancer cells without damaging healthy cells. We have modified their structure to overcome certain types of drug resistance mechanisms by combining the organometallic ruthenium function with potent known org. inhibitors covalently tethered to the arene ring. Various resistance pathways will be discussed, with particular attention to drug inactivation involving glutathione-S-transferase enzymes (GST). Further tumor targeting with sugar-derived ligands will also be discussed.