期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 19, 期 2, 页码 720-727出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201201634
关键词
carboranes; click chemistry; cycloaddition; heterogeneous catalysis; magnetic resonance imaging
资金
- Regione Piemonte
- Nano-IGT project (Converging Technologies)
- ENCITE
- Fondazione Compagnia di San Paolo (Torino)
- EU Action COST [D38]
In this study, the Huisgen reaction has been used to functionalise a carborane cage with a lipophilic moiety and a 1,4,7,10-tetraazacyclododecane1,4,7,10-tetraacetic acid (DOTA) ligand to obtain a new Gd boron neutron-capture therapy (BNCT)/magnetic resonance imaging (MRI) agent. The introduction of the triazole units has been accomplished under both heterogeneous conditions, by the use of a Cu-supported ionic-liquid catalyst, and homogeneous conditions. The ability of the Gd complex of the synthesised ligand to form stable adducts with low-density lipoproteins (LDLs) has been evaluated and then MRI has been performed on tumour melanoma cells incubated in the presence of a Gd-complex/LDL imaging probe. It has been concluded that the high amount of intracellular boron necessary to perform BNCT can be reached even in the presence of a relatively low-boron-containing LDL concentration.
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