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.

• Authors: Boris D Zlatopolskiy, Agnieszka Morgenroth, Elizaveta A Urusova, Cornelia Dinger, Thomas Kull, Manuela Pape, Gerhard Glatting, Sven N Reske
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 17 Pg. 5151-4 (Sep 01 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19632836 (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)