Synthesis and structural diversification of induced pluripotent stem molecules based on polyene macrolactam natural products

2021 Fiscal Year Final Research Report

• Project/Area Number: 19K06990
• 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: Hoshi University
• Principal Investigator: Kanoh Naoki 星薬科大学, 薬学部, 教授 (40317293)
• Co-Investigator(Kenkyū-buntansha): 岩渕 好治 東北大学, 薬学研究科, 教授 (20211766)
• Project Period (FY): 2019-04-01 – 2022-03-31
• Keywords: ポリエンマクロラクタム / 多能性幹分子

Outline of Final Research Achievements

This study aims to design and synthesize polyene macrolactam-based induced pluripotent synthetic small molecules (iPS molecules) that diversify into polycyclic compounds, each having a different skeleton and biological activity in response to various stimuli, such as light irradiation and oxidative conditions, and so on. To apply the reactivity of marine-derived polyene macrolactam heronamide C to the induced pluripotent small molecules, we firstly developed a modular synthetic strategy for the heronamide C-type polyene macrolactams. Then, various heronamide C derivatives were synthesized by using the developed strategy. Evaluation of their reactivity clarified structural factors needed for selective structural diversification.

Free Research Field

有機合成化学

Academic Significance and Societal Importance of the Research Achievements

外的環境に応じて構造や生物活性を変化させる有機小分子の研究は、将来的には患者等の病態・状態に合わせて生物活性や薬理活性を発現するスマートドラッグの開発につながる。本研究はそのような分子の設計と構築を可能とするための第一歩である。また本研究は、アトムエコノミーやステップエコノミーに優れた複雑分子構築法を提案する基礎研究として意義がある。