PET imaging drug distribution after intratumoral injection: the case for (124)I-iododeoxyuridine in malignant gliomas.

Unlabelled: Locoregional administration may yield higher tumor drug concentrations compared with intravenous injection and may reduce the risk of systemic adverse effect. Furthermore, in the case of brain tumors, it may circumvent limited drug delivery imposed by the blood-brain barrier. We used PET to study the retention and spatial distribution of iododeoxyuridine (IUdR), which has been used as a DNA-targeting radiosensitizing drug and which can be charged with therapeutic nuclides.

Synthesis of an o-Carboranyl Derivative of 4-[5-(4-Methyl-1-piperazinyl)-2,5'-bi-1H-benzimidazol-2'-yl]phenol.

Synthesis of an o-carboranyl derivative of 4-[5-(4-methyl-1-piperazinyl)-2,5'-bi-1H-benzimidazol-2'-yl]phenol (1), a candidate for application in boron neutron capture therapy for cancer treatment, is described. Decaborane was introduced into 3-(p-cyanophenoxy)-1-propyne (11) to form 1-(4-cyanophenoxymethyl)-1,2-dicarba-closo-dodecaborane(12) (12), which was transformed into the corresponding imidate 10 in order to be coupled with 4-cyano-o-phenylenediamine (13) to give 1-[4-(5'-cyano-1H-benzimidazol-2'-yl)phenoxymethyl]-1,2-dicarba-closo-dodecaborane(12) (14). The latter was reacted to the related imidate salt 15 and condensed with 5-(4-methyl-1-piperazinyl)-o-phenylenediamine (6) to the title compound 1-{4-[5-(4-methyl-1-piperazinyl)-2,5'-bi-1H-benzimidazol-2'-yl]phenoxymethyl}-1,2-dicarba-closo-dodecaborane(12) (2).