142 Advances in Polymer Science Editorial Board: A. Abe. A.-C ...

224 J. Roovers, B. Comanita
A fourth generation PAMAM dendrimer containing 48 amino groups has
been boronated with Na(CH 3 ) 3 NB 10 H 8 NCO followed by coupling with a thiolated
mono-clonal antibody via a difunctional linking agent as shown in
Scheme 22 [161]. This sequence allows for the incorporation of 1700 boron atoms
per antibody. This level of boronation is potentially sufficient to deliver the
required 10 9 atoms of 10 B to each tumor cell and to sustain a lethal reaction of
10 B with thermal neutrons. Although the boronated dendrimer-antibody conjugate
retained a high in vitro affinity and specificity for the antigens on B16
melanoma cells, in vivo tumor uptake has been disappointing. A similar conjugation
has been performed between boronated PAMAM dendrimer and epidermal
growth factor, a polypeptide with 53 amino acid residues that can be transported
through the brain barrier and target brain tumor cells [162].
6
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