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

Cucciolito, Maria Elena ; De Luca Bossa, Ferdinando ; Esposito, Roberto ; Ferraro, Giarita ; Iadonisi, Alfonso ; Petruk, Ganna LU orcid ; D'Elia, Luigi ; Romanetti, Claudia ; Traboni, Serena and Tuzi, Angela , et al. (2018) In Inorganic Chemistry Frontiers 5(11). p.2921-2933
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... (More)

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.

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publishing date
type
Contribution to journal
publication status
published
in
Inorganic Chemistry Frontiers
volume
5
issue
11
pages
2921 - 2933
publisher
Royal Society of Chemistry
external identifiers
  • scopus:85056276217
ISSN
2052-1553
DOI
10.1039/c8qi00664d
language
English
LU publication?
no
additional info
Publisher Copyright: © the Partner Organisations.
id
d043286e-c5c4-447c-8c4e-0d1230afc39f
date added to LUP
2025-01-21 15:44:50
date last changed
2025-01-22 08:01:37
@article{d043286e-c5c4-447c-8c4e-0d1230afc39f,
  abstract     = {{<p>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.</p>}},
  author       = {{Cucciolito, Maria Elena and De Luca Bossa, Ferdinando and Esposito, Roberto and Ferraro, Giarita and Iadonisi, Alfonso and Petruk, Ganna and D'Elia, Luigi and Romanetti, Claudia and Traboni, Serena and Tuzi, Angela and Monti, Daria Maria and Merlino, Antonello and Ruffo, Francesco}},
  issn         = {{2052-1553}},
  language     = {{eng}},
  number       = {{11}},
  pages        = {{2921--2933}},
  publisher    = {{Royal Society of Chemistry}},
  series       = {{Inorganic Chemistry Frontiers}},
  title        = {{C-Glycosylation in platinum-based agents : a viable strategy to improve cytotoxicity and selectivity}},
  url          = {{http://dx.doi.org/10.1039/c8qi00664d}},
  doi          = {{10.1039/c8qi00664d}},
  volume       = {{5}},
  year         = {{2018}},
}