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 |
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| Affiliation: | 1. Department of Chemistry, Faculty of Science, King Mongkut''s University of Technology Thonburi, Bangkok 10140, Thailand;2. Organic Synthesis Unit, Department of Chemistry, Faculty of Science and Nanotec-CU Center of Excellence on Food and Agriculture Chulalongkorn University, Bangkok 10330, Thailand;3. National Nanotechnology Center, National Science and Technology Development Agency, Pathumthani 12120, Thailand;1. Key Laboratory of Industrial Microbiology, Ministry of Education, Tianjin Key Laboratory of Industry Microbiology, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China;2. Shenogen Pharma Group Ltd, Suite A205, No. 5 Shangdi Kaituo Road, Haidian, Beijing 100085, China;3. Chemo Dynamics, Inc., 3 Crossman Road South, Sayreville, NJ 08872, USA;1. College of Biomedical Engineering, Taiyuan University of Technology, Taiyuan 030024, China;2. Laboratory Animal Center, Shanxi Cancer Institute, Taiyuan 030013, China;3. School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, China;1. Laboratory of Industrial and Synthetic Organic Chemistry (LISOC), Department of Chemistry and Chemical Technologies, University of Calabria, 87036 Arcavacata di Rende, CS, Italy;2. Institute of Crystallography, National Research Council, Via Amendola, 122/O, 70126 Bari, Italy;3. Department of Chemical Sciences, University of Naples “Federico II”, Via Cinthia, 80126 Naples, Italy;4. Department of Chemistry, Life Sciences and Environmental Sustainability (SCVSA), University of Parma, Parco Area delle Scienze, 17/A, 43124 Parma, Italy;5. Department of Industrial Chemistry “T. Montanari”, University of Bologna, Viale Risorgimento 4, 40136 Bologna, BO, Italy;1. Guangdong Provincial Key Laboratory of Fermentation and Enzyme Engineering, Pre-Incubator for Innovative Drugs & Medicine, School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510006, China;2. Department of Pharmacology, Institute of Medical Sciences, Shanghai Jiao Tong University, School of Medicine, 280 South Chongqing Road, Shanghai 200025, China |
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| Abstract: | ![]()
This work reports the synthesis, radiolabeling and preliminary in vitro evaluation of [131I]-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. |
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