title: The hydroboration reaction as a key for a straightforward synthesis of new MRI-NCT agents.
abstract: In this study the hydroboration reaction has been exploited to produce in only four steps a new lipophilic GdBNCT/MRI agent (PB01). As a matter of fact, the formation of a new B–C bond to link the decaborane with the lipophilic moiety greatly simplifies the synthesis of PB01 with respect to the previously reported dual agents. The complexes obtained (PB01a and PB01b) have been fully characterised from the relaxometric point of view and, after disaggregation with HPβCD, both isomers display high affinity for low density lipoproteins (LDLs) that can be exploited as specific carriers of these therapeutic and diagnostic agents for tumour cells. The LDL loading capacity is different for the two isomers. In fact, LDL can be loaded with 75 and 300 units of PB01a and PB01b, respectively, and for this reason, the isomer PB01b results to be the best candidate to perform MRI guided BNCT.
authors: Department of Chemistry, University of Torino, via P. Giuria 7, 10125, Torino, Italy. annamaria.deagostino@unito.it.
authors: Paolo
authors: P
authors: Boggio
authors: Antonio
authors: A
authors: Toppino
authors: Simonetta
authors: S
authors: Geninatti Crich
authors: Diego
authors: D
authors: Alberti
authors: Domenica
authors: D
authors: Marabello
authors: Claudio
authors: C
authors: Medana
authors: Cristina
authors: C
authors: Prandi
authors: Paolo
authors: P
authors: Venturello
authors: Silvio
authors: S
authors: Aime
authors: Annamaria
authors: A
authors: Deagostino
mesh_terms: D001896:Boron Compounds / Q000737:chemistry*; D003287:Contrast Media / Q000138:chemical synthesis* / Q000737:chemistry; D008279:Magnetic Resonance Imaging; D015394:Molecular Structure; D017247:Neutron Capture Therapy
chemical_list: D001896:Boron Compounds; D003287:Contrast Media