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

  

Authors:	Pillarsetty, N.; Cai, S.; Ageyeva, L.; Finn, R. D.; Blasberg, R. G.
Article Title:	Synthesis and evaluation of [18F] labeled pyrimidine nucleosides for positron emission tomography imaging of herpes simplex virus 1 thymidine kinase gene expression
Abstract:	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. © 2006 American Chemical Society.
Keywords:	unclassified drug; genetics; nonhuman; comparative study; positron emission tomography; methodology; animal cell; animal; animals; gene expression; cell line; in vitro study; drug effect; drug screening; enzymology; drug evaluation, preclinical; cell line, tumor; time; time factors; gene expression regulation; chemistry; glioma cell; tumor cell line; rat; positron-emission tomography; chemical structure; molecular structure; thymidine kinase; herpesvirus 1, human; rats; high performance liquid chromatography; structure analysis; fluorine 18; energy; herpes simplex virus 1; reaction analysis; synthesis; stereoisomerism; hsv1 tk gene; gene expression regulation, enzymologic; fluorine radioisotopes; virus gene; fluorine; uracil derivative; 1 bromo 2 deoxy 2 fluorosugar derivative; 2' fluoro 2' deoxy 5 bromovinyl 1 beta dextro arabinofuranosyluracil; 2' fluoro 2' deoxy 5 propyl 1 beta dextro arabinofuranosyluracil; 2' fluoro 2' deoxy 5 trifluoromethyl 1 beta dextro arabinofuranosyluracil; fluoro 1 beta dextro arabinofuranosyluracil derivative; pyrimidine nucleoside; pyrimidine nucleosides
Journal Title:	Journal of Medicinal Chemistry
Volume:	49
Issue:	17
ISSN:	0022-2623
Publisher:	American Chemical Society
Date Published:	2006-08-24
Start Page:	5377
End Page:	5381
Language:	English
DOI:	10.1021/jm0512847
PUBMED:	16913728
PROVIDER:	scopus
DOI/URL:	http://www.scopus.com/inward/record.url?eid=2-s2.0-33747472945&partnerID=40&md5=19daa965dec06040da0fc9deb6829eb4
Notes:	--- - "Cited By (since 1996): 15" - "Export Date: 4 June 2012" - "CODEN: JMCMA" - "Source: Scopus"

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