Synthesis and Evaluation of [18F] Labeled Pyrimidine Nucleosides for Positron Emission Tomography Imaging of Herpes Simplex Virus 1 Thymidine Kinase Gene Expression
| Autor: | Ronald G. Blasberg, Nagavarakishore Pillarsetty, Lyudmila Ageyeva, Shangde Cai, Ronald D. Finn |
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| Rok vydání: | 2006 |
| Předmět: |
Fluorine Radioisotopes
Time Factors Pyrimidine Drug Evaluation Preclinical Herpesvirus 1 Human In Vitro Techniques medicine.disease_cause Thymidine Kinase Chemical synthesis Gene Expression Regulation Enzymologic chemistry.chemical_compound Cell Line Tumor Drug Discovery Gene expression medicine Animals Molecular Structure Stereoisomerism Uracil Pyrimidine Nucleosides In vitro Rats Herpes simplex virus Biochemistry chemistry Cell culture Thymidine kinase Positron-Emission Tomography Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 49:5377-5381 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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