The hydroboration reaction as a key for a straightforward synthesis of new MRI-NCT agents.
Org Biomol Chem
; 13(11): 3288-97, 2015 Mar 21.
Article
em En
| MEDLINE
| ID: mdl-25645198
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 BC 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 HPßCD, 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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Boro
/
Imageamento por Ressonância Magnética
/
Terapia por Captura de Nêutron
/
Meios de Contraste
Idioma:
En
Revista:
Org Biomol Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Itália