Abstract |
Eleven ruthenium-nucleoside conjugates with the general formula [(eta(5)-C5H5)Ru(PP)L][PF6] (PP = 1,2-bis(diphenylphosphino)ethane (Dppe), 2PPh(3), and L = 3-N-(p-cyanobenzyl)thymidine derivative ligand) are reported. Both [(eta(5)-C5H5)Ru(Dppe)N C-R](+) and [(eta(5)-C5H5)Ru(PPh3)(2)N C-R](+) scaffolds exhibit remarkable stability towards hydrolysis. Compounds show high cytotoxicity in HCT116 colon cancer cells, with IC50 values down to 1.0 mu M. Uptake competition experiments with 2 -deoxyadenosine revealed its cellular absorption to be independent of nucleoside transporters. |