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-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoate ([F-18]1, [F-18]MFNBMB) and its corresponding acid 2-(2-[F-18]fluoro-4-nitrobenzamido)-3-methylbutanoic acid ([F-18]2, [F-18]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-[F-18]fluorodeoxyglucose ([F-18]FDG) and O-2-[18F]fluoroethyl- L-tyrosine (L-[18F]FET) in the same model for comparison with our targeting molecules [F-18]1 and [F-18]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 [F-18]1, 2.32, 13.30 for [F-18]2 at 30 min post injection, which were obviously superior to [F-18] FDG and L-[F-18] FET in the same model and demonstrated that [F-18]1 and [F-18]2, especially [F-18]2, were potential PET imaging agents for tumor detection. (C) 2009 Elsevier Ltd. All rights reserved.