Although cytotoxic nucleoside analogues and transition metals were among the first chemotherapeutic agents to be introduced for the medical treatment of cancer, the availability of a combination of both classes of compounds remains scarce, mostly due to synthetic challenges. We propose here a new synthetic methodology for the synthesis of bicyclic modified nucleosides that can be converted into their organometallics. Pursuing the leading structures of hexacarbonyl dicobalt complexes that exhibit activity against human mammary tumor cells, we will synthesize a library of new metallonucleosides and conduct structure-activity relationship studies.