Chapter 12: Development of technetium-99m labelled biomarkers for EGFR-TK using the Tc-tricarbonyl core

The aim of the study was to synthesize and label new biomarkers such as EGFRTK inhibitors using the Tc-tricarbonyl core. 6-amino-4-[(3-bromophenyl)amino]-quinazoline, a compound that is a potent EGFR-TK inhibitor, was selected as one of the lead molecules. This compound was synthesized and distributed to other members, in order to perform coupling with the bifunctional agents. Furthermore, it was derivatized with various chelating moieties and their Re-tricarbonyl complexes were prepared and characterized by infrared spectroscopy and nuclear magnetic resonance spectroscopy. Analogous 99mTc-tricrbonyl complexes were also prepared. In vitro studies of the ligands as well as of the Re-tricarbonyl complexes with A431 cells demonstrated their ability to inhibit cell growth as well as to inhibit phosphorylation in the presence of at least 1mM of the compounds studied. (author)