Peer-reviewed veterinary case report
2-Fluoropyridine prosthetic compounds for the 18F labeling of bombesin analogues.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2013
- Authors:
- Inkster, James et al.
- Affiliation:
- TRIUMF · Canada
Abstract
Acetylene-bearing 2-[(18)F]fluoropyridines [(18)F]FPy5yne and PEG-[(18)F]FPyKYNE were prepared via efficient nucleophilic heteroaromatic [(18)F]fluorination of their corresponding 2-trimethylammoniumpyrdinyl precursors. The prosthetic groups were conjugated to azide- and PEG3-modified bombesin(6-14) analogues via copper-catalyzed azide-alkyne cycloaddition couplings to yield mono- and di-mini-PEGylated ligands for PET imaging of the gastrin- releasing peptide receptor. The PEG3- and PEG2/PEG3-bearing (18)F peptides showed decreased lipophilicity relative to an analogous non-mini-PEGylated (18)F peptide. Assessment of water-soluble peptide pharmacokinetics and tumour-targeting capabilities in a mouse model of prostate cancer is currently underway.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/23683595/