Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.
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.
Zlatopolskiy
Boris D
BD
Klinik für Nuklearmedizin, Ulm University, Albert-Einstein-Allee 23, Ulm, Germany.
Morgenroth
Agnieszka
A
Urusova
Elizaveta A
EA
Dinger
Cornelia
C
Kull
Thomas
T
Pape
Manuela
M
Glatting
Gerhard
G
Reske
Sven N
SN
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry; D045744:Cell Line, Tumor; D033721:Equilibrative Nucleoside Transporter 1 / Q000378:metabolism*; D005434:Flow Cytometry; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D013872:Thionucleosides / Q000138:chemical synthesis / Q000737:chemistry*
D001549:Benzamides; D033721:Equilibrative Nucleoside Transporter 1; D005456:Fluorescent Dyes; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; C438649:SLC29A1 protein, human; D013872:Thionucleosides; C066257:5'-S-(2-aminoethyl)-N(6)-(4-nitrobenzyl)-5'-thioadenosine; D000241:Adenosine