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Organoruthenium(II) Nucleoside Conjugates as Colon Cytotoxic Agents

Abstract

Eleven ruthenium-nucleoside conjugates of general formula [(η5-C5H5)Ru(PP)L][PF6] (PP = Dppe, 2PPh3, L = 3-N-(p-cyanobenzyl)thymidine derivative ligand) are reported. Both [(η5-C5H5)Ru(Dppe)N≡C-R]+ and [(η5-C5H5)Ru(PPh3)2N≡C-R]+ scaffold demonstrate a remarkable stability towards hydrolysis. Compounds show high cytotoxicity in HCT116 colon cancer cells, with IC50 values down to 1.01 µM. Uptake competition experiments with 2’-deoxyadenosine revealed its cellular absorption to be independent of nucleoside transporters.

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Publication details

The article was received on 05 Sep 2018, accepted on 27 Nov 2018 and first published on 27 Nov 2018


Article type: Paper
DOI: 10.1039/C8NJ04515A
Citation: New J. Chem., 2018, Accepted Manuscript
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    Organoruthenium(II) Nucleoside Conjugates as Colon Cytotoxic Agents

    P. Florindo, D. Pereira, P. Borralho, M. F. Minas da Piedade, M. C. Oliveira, A. Dias, C. Rodrigues and A. C. Fernandes, New J. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8NJ04515A

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