Organoruthenium(ii) nucleoside conjugates as colon cytotoxic agents. (14th December 2018)

• Record Type: Journal Article
• Authors: Florindo, Pedro R.; Pereira, Diane M.; Borralho, Pedro M.; Piedade, M. F. M.; Oliveira, M. Conceição; Dias, Ana M.; Rodrigues, Cecília M. P.; Fernandes, Ana C.
• Is Part Of: New journal of chemistry. Volume 43:Number 3(2019)
• Page Start: 1195
• Page End: 1201
• Publication Date: 2018-12-14
• Subjects: Chemistry -- Periodicals; Chimie -- Périodiques; 540
• DOI: 10.1039/c8nj04515a
• Languages: English
• ISSNs: 1144-0546

Abstract

Abstract : Eleven organoruthenium(ii ) nucleoside conjugates are reported, showing high cytotoxicity in HCT116 colon cancer cells and independent uptake of nucleoside transporters. Abstract : Eleven ruthenium-nucleoside conjugates with the general formula [(η 5 -C5 H5 )Ru(PP)L][PF6 ] (PP = 1, 2-bis(diphenylphosphino)ethane (Dppe), 2PPh3, and L = 3- N -( p -cyanobenzyl)thymidine derivative ligand) are reported. Both [(η 5 -C5 H5 )Ru(Dppe)NC-R] + and [(η 5 -C5 H5 )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 μM. Uptake competition experiments with 2′-deoxyadenosine revealed its cellular absorption to be independent of nucleoside transporters.