Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues
| Autor: | Gerhard Glatting, Sven N. Reske, Thomas Kull, Cornelia Dinger, Elizaveta A. Urusova, Manuela Pape, Agnieszka Morgenroth, Boris D. Zlatopolskiy |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Adenosine
HL60 Clinical Biochemistry Pharmaceutical Science Tumor cells Nucleoside transporter Biochemistry Flow cytometry Equilibrative Nucleoside Transporter 1 Iodine Radioisotopes chemistry.chemical_compound In vivo Cell Line Tumor Drug Discovery medicine Humans Molecular Biology Fluorescent Dyes Thionucleosides medicine.diagnostic_test biology Organic Chemistry medicine.disease Flow Cytometry In vitro Leukemia chemistry Active compound Positron-Emission Tomography Benzamides biology.protein Molecular Medicine Radiopharmaceuticals |
| Zdroj: | Bioorganicmedicinal chemistry letters. 19(17) |
| ISSN: | 1464-3405 |
| Popis: | Three new potential hENT1 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. 131I-5 showed high hENT1-specific binding (up to 54% ID) to 6 from 7 tested tumor cell lines and was chosen for further in vivo study. |
| Databáze: | OpenAIRE |
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