An improved synthesis of 1,3,5-triazine-based imaging agents utilizing peptides as targeting groups has been developed.  By controlling the temperature, 2,4,6-trisubstituted triazines can be prepared by sequential selective addition of nucleophiles in a one-pot synthesis with high yields.   The peptide bombesin and its associated receptor, Gastrin-releasing peptide (GRP), have been shown to play a role in cancer. GRPR targeting bombesin analogs were 'clicked' onto the triazine core by CuAAC (copper catalyzed azide-alkyne cycloaddition) reaction. The multivalent and monomeric  bombesin derivatives were compared regarding their affinity towards the GRPR receptors in an in vitro binding assay.  These agents can be further functionalized at the triazine core with chelates for radiometals such as Cu-64 or Ga-68 for PET imaging, or with fluorescent dyes for optical imaging. The in vivo evaluation of these novel radio-pharmaceuticals are under investigation.

Incorporation of bombesin into a triazine-based platform for the development of targeted imaging probes

246th National Meeting (2013)

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