Evaluation of silicon-astatine exchange reaction by kinetics approach and its applications to the development of alpha-emitting therapeutic agents
| Project/Area Number |
17K10459
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | National Institutes for Quantum and Radiological Science and Technology |
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Principal Investigator |
Watanabe Shigeki 国立研究開発法人量子科学技術研究開発機構, 高崎量子応用研究所 放射線生物応用研究部, 主幹研究員(定常) (10450305)
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| Co-Investigator(Kenkyū-buntansha) |
山田 圭一 群馬大学, 大学院理工学府, 准教授 (70323334)
羽場 宏光 国立研究開発法人理化学研究所, 仁科加速器科学研究センター, チームリーダー (60360624)
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | アスタチン-211 / 標的α線治療 / ケイ素―ハロゲン交換反応 / アミノ酸 / アスタチン / 放射性ハロゲン / ケイ素ーハロゲン交換反応 / RI標識 / α線治療 / 標的アイソトープ治療 / α線 / ケイ素 / 放射性薬剤 |
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| Outline of Final Research Achievements |
Astatine-211 is one of the promising radionuclides for the Targeted Alpha Therapy (Radionuclide therapy using alpha-emitting radionuclides). The aims of this study are to evaluate the usefulness of silicon-astatine (Si-At) exchange reaction (electrophilic desilylation) by kinetic approach and to synthesize astatinated compounds via the Si-At exchange reaction. We have successfully synthesized an astatinated amino acid (phenylalanine) and benzylguanidine (MABG) in a good yield which is better than those by the conventional astatinated method. Therefore, this study revealed that the Si-At exchange reaction is quite useful for the synthesis of astatinated compounds for the Targeted Alpha Therapy.
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| Academic Significance and Societal Importance of the Research Achievements |
標的α線治療は、β線を用いる従来の治療法よりも高い効果が期待されることから、これまで治療が難しかった疾患の治療が期待できる。本研究で検討したケイ素―アスタチン交換反応は、At-211標識化合物を簡便かつ高収率で合成できるため、今後、これまで合成が難しかった化合物の合成が可能になり、ひいては新たな標的α線治療用薬剤の開発につながることが期待できる。
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Report
(4 results)
Research Products
(12 results)
