Construction of Compound Library Based on the High Oxidation Skeleton of Meroterpenoids and Application for Anti-tumor Drug Design

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K06574
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
• Research Institution: University of Toyama
• Principal Investigator: Matsuya Yuji 富山大学, 学術研究部薬学・和漢系, 教授 (50255858)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: 抗癌剤 / 天然物 / アンドラスチン / 医薬設計

Outline of Final Research Achievements

Based on the meroterpenoid natural products, novel drug design with simplified pharmacophore structures was performed, and the relationship between oxidation states and biological activities was investigated. The synthetic route for the key intermediates toward various designed structures could be developed, and the methodology of the required oxidation reaction of the designed skeleton could be found in this investigation. Optimized reaction conditions for each efficient chemical transformations could be established.

Free Research Field

有機化学

Academic Significance and Societal Importance of the Research Achievements

抗癌作用が期待されるアンドラスチンというメロテルペノイドのCD環部を抽出して、構造単純化した新規誘導体の合成経路開拓に、道筋をつけることができた。構造簡略化により、合成化学的なアプローチが容易となるものである。これらの結果は、新規抗癌性化合物を探索するための基盤として、今後の抗癌剤創薬への展開が期待できるものである。