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2021 Fiscal Year Final Research Report

Design, Synthesis and Evaluation of Biologically Active Molecules Based on Ring Strain

Research Project

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Project/Area Number 19H03350
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Review Section Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
Research InstitutionKyoto University

Principal Investigator

Takasu Kiyosei  京都大学, 薬学研究科, 教授 (10302168)

Co-Investigator(Kenkyū-buntansha) 服部 明  京都大学, 薬学研究科, 准教授 (50300893)
山岡 庸介  京都大学, 薬学研究科, 助教 (60624723)
Project Period (FY) 2019-04-01 – 2022-03-31
Keywordsひずみ分子 / 精密有機合成 / 小員環 / 中員環 / ADC / 刺激応答
Outline of Final Research Achievements

We made clear that strained molecules showing characteristic reactivity and conformations due to ring distortion can be molecular skeletons that open up new chemical spaces in the fields of drug discovery and materials science. In particular, we developed small ring compounds that undergo molecular transformation stimulated by hypochlorous acid produced by neutrophils, and established the basis for the development of probes to observe in vivo stimuli. In addition, we synthesized ADCs (antibody-drug conjugates) with alkaloids as payloads that exhibit potent anticancer activity and demonstrated significant activity in vitro.

Free Research Field

有機化学

Academic Significance and Societal Importance of the Research Achievements

環ひずみをもつ分子は、特徴あるコンホメーションや化学反応性を提示しうる創薬プラットホーム分子、有機材料プラットホーム分子になることを、より一層明確にすることができた。特に、小員環の縮環シクロブテンは微量反応活性化合物のtrans-シクロアルケンとの平衡混合物であることを利用し、生体直交型クリック反応剤として働くことことを発見するとともに、ADCなどの新創薬モダリティの創製に利用できることを明確にした。

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Published: 2023-01-30  

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