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C-Glycosylation in platinum-based agents: a viable strategy to improve cytotoxicity and selectivity

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Abstract

Novel coordinatively saturated platinum(II) compounds bearing C-linked carbohydrates were synthesized and characterized. The complexes exhibit bipyramidal trigonal geometry with a bidentate nitrogen ligand and ethylene in the equatorial plane. The axial positions are occupied by a halide ligand X and a D-galactose or D-glucose derivative, linked either via C1 or C6. The compounds were designed for evaluation of the biological activity because they combine the steady coordinative saturation, the beneficial action of the modular sugar moiety and the organometallic nature of the Pt-sugar linkage, which is expected to be stable in the biological media, until the target is reached. The newly synthesized molecules were stable in mixed DMSO/aqueous solvents, able to bind DNA in vitro and exhibited a selective cytotoxic activity on cancer cells through apoptosis activation.

Graphical abstract: C-Glycosylation in platinum-based agents: a viable strategy to improve cytotoxicity and selectivity

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Publication details

The article was received on 08 Jul 2018, accepted on 29 Sep 2018 and first published on 01 Oct 2018


Article type: Research Article
DOI: 10.1039/C8QI00664D
Citation: Inorg. Chem. Front., 2018, Advance Article
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    C-Glycosylation in platinum-based agents: a viable strategy to improve cytotoxicity and selectivity

    M. E. Cucciolito, F. De Luca Bossa, R. Esposito, G. Ferraro, A. Iadonisi, G. Petruk, L. D'Elia, C. Romanetti, S. Traboni, A. Tuzi, D. M. Monti, A. Merlino and F. Ruffo, Inorg. Chem. Front., 2018, Advance Article , DOI: 10.1039/C8QI00664D

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