CuIIand AuIIIComplexes with Glycoconjugated Dithiocarbamato Ligands for Potential Applications in Targeted Chemotherapy
| Autor: | Alberto Gambalunga, Federica Chiara, Barbara Biondi, Dolores Fregona, Chiara Nardon, Leonardo Brustolin, Andrea Trevisan, Nicolò Pettenuzzo, Elisa Coltri |
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| Rok vydání: | 2019 |
| Předmět: |
dithiocarbamates
medicine.medical_treatment carbohydrates metal complexes 01 natural sciences Biochemistry In vivo Drug Discovery medicine Moiety Monosaccharide Cytotoxic T cell carbohydrates · copper · gold · dithiocarbamates · metal complexes General Pharmacology Toxicology and Pharmaceutics Lipid bilayer Pharmacology chemistry.chemical_classification Chemotherapy 010405 organic chemistry Organic Chemistry gold Combinatorial chemistry Warburg effect In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry copper Molecular Medicine |
| Zdroj: | ChemMedChem 14 (2019): 1162–1172. doi:10.1002/cmdc.201900226 info:cnr-pdr/source/autori:Pettenuzzo, Nicolo; Brustolin, Leonardo; Coltri, Elisa; Gambalunga, Alberto; Chiara, Federica; Trevisan, Andrea; Biondi, Barbara; Nardon, Chiara; Fregona, Dolores/titolo:Cu-II and Au-III Complexes with Glycoconjugated Dithiocarbamato Ligands for Potential Applications in Targeted Chemotherapy/doi:10.1002%2Fcmdc.201900226/rivista:ChemMedChem (Print)/anno:2019/pagina_da:1162/pagina_a:1172/intervallo_pagine:1162–1172/volume:14 |
| ISSN: | 1860-7187 1860-7179 |
| Popis: | This work is focused on the synthesis, characterization, and preliminary biological evaluation of bio-conjugated Au-III and Cu-II complexes with the aim of overcoming the well-known side effects of chemotherapy by improving the selective accumulation of an anticancer metal payload in malignant cells. For this purpose, carbohydrates were chosen as targeting agents, exploiting the Warburg effect that accounts for the overexpression of glucose-transporter proteins (in particular GLUTs) in the phospholipid bilayer of most neoplastic cells. We linked the dithiocarbamato moiety to the C1 position of three different monosaccharides: d-glucose, d-galactose, and d-mannose. Altogether, six complexes with a 1:2 metal-to-ligand stoichiometry were synthesized and in vitro tested as anticancer agents. One of them showed high cytotoxic activity toward the HCT116 colorectal human carcinoma cell line, paving the way to future in vivo studies aimed at evaluating the role of carbohydrates in the selective delivery of whole molecules into cancerous cells. |
| Databáze: | OpenAIRE |
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