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ID: ALA1155315
Journal: Bioorg Med Chem Lett
Title: Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.
Authors: Zlatopolskiy BD, Morgenroth A, Urusova EA, Dinger C, Kull T, Pape M, Glatting G, Reske SN.
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.
CiteXplore: 19632836