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

作者信息

Zlatopolskiy Boris D, Morgenroth Agnieszka, Urusova Elizaveta A, Dinger Cornelia, Kull Thomas, Pape Manuela, Glatting Gerhard, Reske Sven N

机构信息

Klinik für Nuklearmedizin, Ulm University, Albert-Einstein-Allee 23, Ulm, Germany.

出版信息

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5151-4. doi: 10.1016/j.bmcl.2009.07.017. Epub 2009 Jul 9.

DOI:10.1016/j.bmcl.2009.07.017
PMID:19632836
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.

摘要

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