Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.
Bioorg Med Chem Lett
; 19(17): 5151-4, 2009 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tionucleosídeos
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Benzamidas
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Adenosina
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Compostos Radiofarmacêuticos
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Transportador Equilibrativo 1 de Nucleosídeo
Limite:
Humans
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article