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Issue 3, 2019
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Organoruthenium(II) nucleoside conjugates as colon cytotoxic agents

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Abstract

Eleven ruthenium-nucleoside conjugates with the general formula [(η5-C5H5)Ru(PP)L][PF6] (PP = 1,2-bis(diphenylphosphino)ethane (Dppe), 2PPh3, and L = 3-N-(p-cyanobenzyl)thymidine derivative ligand) are reported. Both [(η5-C5H5)Ru(Dppe)N[triple bond, length as m-dash]C-R]+ and [(η5-C5H5)Ru(PPh3)2N[triple bond, length as m-dash]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.

Graphical abstract: Organoruthenium(ii) nucleoside conjugates as colon cytotoxic agents

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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., 2019,43, 1195-1201

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    Organoruthenium(II) nucleoside conjugates as colon cytotoxic agents

    P. R. Florindo, D. M. Pereira, P. M. Borralho, M. F. M. Piedade, M. C. Oliveira, A. M. Dias, C. M. P. Rodrigues and A. C. Fernandes, New J. Chem., 2019, 43, 1195
    DOI: 10.1039/C8NJ04515A

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