Synthesis and evaluation of [18F] labeled pyrimidine nucleosides for positron emission tomography imaging of herpes simplex virus 1 thymidine kinase gene expression

Article abstract of DOI:10.1021/jm0512847

Synthesis of three novel 2′-deoxy-2′-[¹⁸F]fluoro-1- β-D-arabinofuranosyluracil derivatives [¹⁸F]FPAU, [ ¹⁸F]-FBrVAU, and [¹⁸F]FTMAU is reported. The compounds were synthesized by coupling of 1-bromo-2-deoxy-2-fluoro sugars with corresponding silylated uracil derivatives. In vitro cell uptake indicated that all three compounds are taken up selectively in RG2TK+ cells with negligible uptake in RG2 cells. The results indicate that [¹⁸F]FBrVAU and [ ¹⁸F]FTMAU have better uptake profiles in comparison to [ ¹⁸F]FPAU and have potential as PET probes for imaging HSV1-tk gene expression.