Synthesis, radiosynthesis, and in vitro evaluation of [131I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide as a potential tumor imaging agent.
This work reports the synthesis, radiolabeling and preliminary in vitro evaluation of [(131)I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide. The tributylstannylprecursor was synthesized with a yield of 38%. Radiolabeling was performed using an electrophilic iododestannylation. Tracer yield was 94%, radiochemical purity was >95%. The tracer showed high uptake in MCF-7 breast cancer cell line and therefore will be evaluated further.
Xu
Yu Ping
YP
The Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, Wuxi 214063, China.
Yang
Min
M
Pan
Dong Hui
DH
D001549:Benzamides / Q000138:chemical synthesis*; D045744:Cell Line, Tumor; D006801:Humans; D007457:Iodine Radioisotopes; D007546:Isoquinolines / Q000138:chemical synthesis*; D009682:Magnetic Resonance Spectroscopy; D009369:Neoplasms / Q000000981:diagnostic imaging*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D021241:Spectrometry, Mass, Electrospray Ionization
C539911:5-iodo-N-(2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl)-2-methoxybenzamide; D001549:Benzamides; D007457:Iodine Radioisotopes; D007546:Isoquinolines; D019275:Radiopharmaceuticals