Nuclide therapy for cancer is based on the selective delivery of nuclide bearing compounds to tumour cells. Radionuclides, such as ¹²⁵I, may be used, as well as stable isotopes, such as ¹⁰B, which is activated on site by an external neutron source. The second methodology is used in Boron Neutron Capture Therapy, which utilises the cytotoxic effect from the neutron capture reaction ¹⁰B(n,α)⁷Li. With this background in mind, nuclide bearing amino acids, nucleosides, and isoquinolines have been synthesised.

Carborane containing analogues of phenylalanine were asymmetrically synthesised using Oppolzer's camphor-derived chiral handle. The (R)- and (S)-[3-(1,7-dicarba-closo-dodecaborane(12)-1-yl)-2-aminopropanoic acid] (meta-carboranylalanine), were obtained in >99 % enantiomeric purity. The (S)-Boc-ortho-carboranylalanine was obtained in two steps from (2S,2'S)-N-(3'(1",2"-dicarba-closo-dodecaborane(12)-1"-yl)-2'-aminopropanoyl)bornane-10,2-sultam.

Three carborane containing thymidine derivatives 3'-O-(o-carboran-1-ylmethyl)thymidine, 7-(thymidine-3'-ylmethyl)dodecahydro-7,8-dicarba-nino-undecaborate, and 3'-O-(p-carboran-1-ylpropyl)thymidine were synthesised from thymidine. In vitro evaluation regarding enzymatic phosphorylation is described.

Three iodo-analogues of the peripheral benzodiazepine receptor (PBR) ligand PK 11195, namely the isoquinoline derivatives N-Methyl-N-(1-methylpropyl)-1-(2-iodo phenyl)isoquinoline-3-carboxamide, N-Methyl-N-(1-methylpropyl)-1-(3-iodophenyl) isoquinoline-3-carboxamide, and N-Methyl-N-(1-methylpropyl)-1-(4-iodophenyl)isoquinoline -3-carboxamide were synthesised and radiolabelled with ¹²⁵I.

The carborane containing isoquinoline derivative N-Methyl-N-(1-methylpropyl)-l-[2'-(l"-7"-dicarba-closo-dodecaborane(12)-l"-yl)ethyl]isoquinoline-3-carboxamide was synthesised as a potential PBR-ligand.