AbstractIn this research, we are working on development of the chemical synthesis of dimeric or pseudo-dimeric natural products possessing complex structures, which are expected to contribute to middle-molecular drug discovery. The chemical synthesis of these dimeric natural products requires the development of novel methods for linking two highly complex units. We have focused on their proposed biosynthetic pathways, including enzyme-mediated oxidative coupling of the corresponding monomers. Inspired by the biosynthesis, we have developed a coupling method using an enzyme-mimetic catalyt. Through extensive investigations of various iron catalysts, we found that carboxylated iron phthalocyanine catalysts exhibit higher reactivity and chemoselectivity compared to conventional iron catalysts. Based on the established method, we are now advancing the integrated chemical synthesis of various dimeric compounds with diverse skeletons. Furthermore, we plan to conduct research of drug discovery through the evaluation of biological activities of the synthesized natural and pseudo-natural compounds.はじめに有機合成化学による創薬は，医薬品を安価かつ大量に供給可能であり，世界的な感染症のパンデミックへの対応や医療費高騰の抑制，経済格差の大きい地域における疾病の治療などにも有効である．しかし，20 世紀において創薬の主流であった低分子医薬品の開発は，シード化合物の枯渇問題から，その継続的な発展は年々ハードルが高くなり，新たな標的化合物群の探索と革新的な科学技術の創出が求められている．本研究では，新たな標的化合物群として，二つの類似した骨格からなる二量体型天然物に着目した．二量体化合物は，その多くが単量体と比べ強力な生物活性や特異な作用機序を有東北大学大学院薬学研究科医薬製造化学分野・准教授Graduate School of Pharmaceutical Sciences, Tohoku University植田 浩史Hirofumi Ueda― 83 ―高次構造を有する二量体型天然物の統合的合成を基盤とした創薬研究Drug discovery research based on integrated synthesis of dimeric natural products with complex structures
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