Synthesis and biological evaluation of 2-(3,4-dimethoxyphenyl)-6-(2-[18F]fluoroethoxy)benzothiazole ([18F]FEDBT) for PET imaging of breast cancer |
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Authors: | Geng-Ying Li Daria D Vaulina Jia-Je Li Olga S Fedorova Hsin-Ell Wang Ren-Shyan Liu Raisa N Krasikova Chuan-Lin Chen |
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Institution: | 1. Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, Taiwan;2. N.P. Bechtereva Institute of Human Brain, Russian Academy of Science, Saint-Petersburg, Russian Federation;3. Molecular and Genetic Imaging Core/Taiwan Mouse Clinic, National Comprehensive Mouse Phenotyping and Drug Testing Center, Taipei, Taiwan;4. National PET/Cyclotron Center and Department of Nuclear Medicine, Taipei Veterans General Hospital, Taipei, Taiwan;5. St.-Petersburg State University, Saint-Petersburg, Russian Federation |
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Abstract: | Given the ever-present demand for improved PET radiotracer in oncology imaging, we have synthesized 2-(3,4-dimethoxyphenyl)-6-(2-18F]fluoroethoxy)benzothiazole (18F]FEDBT), a fluorine-18-containing fluoroethylated benzothiazole to explore its utility as a PET imaging tracer. 18F]FEDBT was prepared via kryptofix-mediated nucleophilic substitution of the tosyl group precursor. Fractionated ethanol-based solid-phase (SPE cartridge-based) purification afforded 18F]FEDBT in 60% radiochemical yield (EOB), with radiochemical purity in excess of 98% and the specific activity was 35 GBq/μmol. The radiotracer displayed clearly higher cellular uptake ratio in various breast cancer cell lines MCF7, MDA-MB-468 and MDA-MB-231. However, both biodistribution and microPET studies have showed an higher abdominal accumulation of 18F]FEDMBT and the tumor/muscle ratio of 1.8 was observed in the MDA-MB-231 xenograft tumors mice model. Further the lipophilic improvement is needed for the reducement of hepatobilliary accumulation and to promote the tumor uptake for PET imaging of breast cancer. |
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Keywords: | Breast cancer Positron emission tomography Fluorine-18 Benzothiazole |
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