Synthesis and evaluation of novel F-18 labeled fluoroarylvaline derivatives: Potential PET imaging agents for tumor detection

Two F-18 labeled fluoroarylvaline derivatives, methyl 2-(2-[18F]fluoro-4-nitrobenzamido)-3-methylbutanoate ([18F]1, [18F]MFNBMB) and its corresponding acid 2-(2-[18F]fluoro-4-nitrobenzamido)-3-methylbutanoic acid ([18F]2, [18F]FNBMBA), have been designed and synthesized, respectively, by our team. Meanwhile, we research on their biodistributions in mice model bearing S 180 tumor. Furthermore, we also carried out the biological evaluations of 2-[18F]fluorodeoxyglucose ([18F]FDG) and O-2-[18F]fluoroethyl-l-tyrosine (l-[18F]FET) in the same model for comparison with our targeting molecules [18F]1 and [18F]2. Excitingly, the tumor/blood (T/Bl) and tumor/brain (T/Br) ratios were 2.91, 7.06 at 30 min, 3.44, 5.61 at 60 min post injection for [18F]1, 2.32, 13.30 for [18F]2 at 30 min post injection, which were obviously superior to [18F]FDG and l-[18F]FET in the same model and demonstrated that [18F]1 and [18F]2, especially [18F]2, were potential PET imaging agents for tumor detection.

Graphical abstractTwo novel tumor imaging agents for PET are reported. Research on their biodistributions was evaluated with tumor-bearing mice. The agents were obviously superior to [18F]FDG and l-[18F ]FET studied in the same model.Figure optionsDownload full-size imageDownload as PowerPoint slide