2021 Fiscal Year Final Research Report
Construction of silicon atom-containing meroterpenoid-like compounds and expansion of chemical space.
Project/Area Number |
19K06989
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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Research Institution | Tohoku University |
Principal Investigator |
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Project Period (FY) |
2019-04-01 – 2022-03-31
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Keywords | 天然物 / ケイ素原子 / メロテルペノイド / デカリン / ケミカルスペース / 創薬シーズ |
Outline of Final Research Achievements |
Natural products have been playing an important role in drug discovery research. In recent years, however, the percentage of natural products with novel structures obtained from nature has been decreasing. To address this issue, we have devised a method to incorporate silicon atoms, which are not incorporated into the biosynthetic pathway, into a molecular framework. In this study, our aim is to construct synthetic routes of silicon atom-containing meroterpenoid-like compounds. As a result, we achieved not only construction of silicon atom-containing meroterpenoid-like compounds, but also a synthetic method for obtaining tetrasubstituted silanes by means of removing the gem-diphenyl group on the silicon atom and a nucleophilic addition reaction. Our study is expected to be applied to the expansion of new chemical space and drug discovery research in the future.
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Free Research Field |
天然物化学,有機合成化学
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Academic Significance and Societal Importance of the Research Achievements |
天然物は創薬研究や新規骨格創出において重要な役割を担ってきたが,近年では新規性の高い構造を有した化合物の取得割合が減少傾向にある.そこで,研究代表者らは新たな創薬シーズの獲得のため, 生物の生合成によっては得られない構造多様な化合物の創出を目的に研究を行っている. 本研究では, ケイ素原子を分子骨格中に組み込むことによって新規骨格を創出することを試みた.その結果,研究代表者らは,ケイ素原子含有メロテルペノイド様化合物群の創出を達成した.これらは現在までに報告例がなく,前例のない骨格であるため学術的価値が高い.さらに,詳細な生物活性評価を行うことで新たな創薬シーズを提供できると期待している.
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