A Carborane Derivative “Click” Reaction under Heterogeneous Conditions for the Synthesis of a Promising Lipophilic MRI/GdBNCT Agent

In this work the Huisgen reaction has been used to functionalise a carborane cage with a lipophilic moiety and DOTA ligand in order to obtain a new GdBNCT/MRI agent. The introduction of the triazole units has been accomplished both in heterogeneous, by the use of Cu-SILC catalyst, and in homogeneous conditions. The ability of the Gd complex of the synthesised ligand to form stable adducts with 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.