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Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.

Abstract
Three new potential hENT(1) inhibitors suitable for labeling with PET/SPECT radioisotopes were prepared from an advanced intermediate 4. They were tested for their capability to inhibit binding of SAENTA-fluorescein to HL60 leukemia cells in flow cytometry assay and SAENTA-I (5) was determined to be the most active compound. (131)I-5 showed high hENT(1)-specific binding (up to 54% ID) to 6 from 7 tested tumor cell lines and was chosen for further in vivo study.
AuthorsBoris D Zlatopolskiy, Agnieszka Morgenroth, Elizaveta A Urusova, Cornelia Dinger, Thomas Kull, Manuela Pape, Gerhard Glatting, Sven N Reske
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 17 Pg. 5151-4 (Sep 1 2009) ISSN: 1464-3405 [Electronic] England
PMID19632836 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Benzamides
  • Equilibrative Nucleoside Transporter 1
  • Fluorescent Dyes
  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • SLC29A1 protein, human
  • Thionucleosides
  • 5'-S-(2-aminoethyl)-N(6)-(4-nitrobenzyl)-5'-thioadenosine
  • Adenosine
Topics
  • Adenosine (analogs & derivatives, chemical synthesis, chemistry)
  • Benzamides (chemical synthesis, chemistry)
  • Cell Line, Tumor
  • Equilibrative Nucleoside Transporter 1 (metabolism)
  • Flow Cytometry
  • Fluorescent Dyes (chemistry)
  • Humans
  • Iodine Radioisotopes (chemistry)
  • Positron-Emission Tomography
  • Radiopharmaceuticals (chemical synthesis, chemistry)
  • Thionucleosides (chemical synthesis, chemistry)

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