Collect. Czech. Chem. Commun. 2002, 67, 913-935

Polyhedral Boron Compounds as Potential Linkers for Attachment of Radiohalogens to Targeting Proteins and Peptides. A Review

Vladimir Tolmacheva,b and Stefan Sjöberga,*

a Department of Organic Chemistry, Uppsala University, Box 531, SE-751 21 Uppsala, Sweden
b Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, SE-751 85 Uppsala, Sweden


Polyhedral boron clusters (PBC) are three-dimensional inorganic aromatic systems. Some of them can easily be halogenated, and the halogen-boron bond in such systems is very strong. We consider the use of PBC as linkers for attachment of radioactive halogen isotopes to tumor-targeting proteins and peptides. In this review the major preconditions for such applications, such as biological considerations, knowledge concerning coupling chemistry and radiolabeling of PBC, are described. A review with 90 references.

Keywords: Tumour targeting; 123I; 125I; 76Br; 211At; Polyhedral boron clusters; Prosthetic groups; Boranes; Carboranes; Isotope labelling.

References: 90 live references.