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

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
  • 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)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!

Choose Username:
Verify Password: