Abstract
Synthesis of three novel 2'-deoxy-2'-[18F]fluoro-1-beta-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.
Publication types
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Comparative Study
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Cell Line, Tumor
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Drug Evaluation, Preclinical
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Fluorine Radioisotopes
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Gene Expression Regulation, Enzymologic / drug effects*
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Herpesvirus 1, Human / drug effects
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Herpesvirus 1, Human / enzymology*
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In Vitro Techniques
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Molecular Structure
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Positron-Emission Tomography / methods*
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Pyrimidine Nucleosides / chemical synthesis*
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Pyrimidine Nucleosides / chemistry
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Pyrimidine Nucleosides / pharmacokinetics*
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Rats
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Stereoisomerism
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Thymidine Kinase / drug effects
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Thymidine Kinase / genetics*
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Time Factors
Substances
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Fluorine Radioisotopes
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Pyrimidine Nucleosides
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Thymidine Kinase