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抗癌剤テロメスタチンを母骨格とするヒ合物ライブラリーの合成研究

Research Project

Project/Area Number 18032028
Research Category

Grant-in-Aid for Scientific Research on Priority Areas

Allocation TypeSingle-year Grants
Review Section Science and Engineering
Research InstitutionTokyo Institute of Technology

Principal Investigator

土井 隆行  Tokyo Institute of Technology, 大学院・理工学研究科, 准教授 (90212076)

Project Period (FY) 2006 – 2007
Project Status Completed (Fiscal Year 2007)
Budget Amount *help
¥6,400,000 (Direct Cost: ¥6,400,000)
Fiscal Year 2007: ¥3,200,000 (Direct Cost: ¥3,200,000)
Fiscal Year 2006: ¥3,200,000 (Direct Cost: ¥3,200,000)
Keywordsテロメスタチン / テロメアーゼ阻害剤 / 環状ペプチド / ヘテロ環
Research Abstract

本研究では,癌細胞の増殖能を司るテロメアーゼの阻害剤として,微生物の代謝産物から単離されたtelomestatin(1)の各種誘導体ライブラリーの効率的合成法を開発し,telomestatinの分子レべルでの機能解明,およびさらに強力な阻害剤開発に必要な知見を獲得することを目的とする。1は2つのメチルオキサゾール,5つのオキサゾール,およびチアゾリンが連続的に連結し環構造を有する特異な構造を有する。(R)-telomestatinの全合成に引き続きその鏡像体の合成を行った。その間、大環状の環化においてシステイン残基がエピ化するという問題を解決し、望む全合成を達成した。両鏡像体のCDスペクトルと天然物のスペクトルとの比較により、天然物がR体であると決定した。

Report

(2 results)
  • 2007 Annual Research Report
  • 2006 Annual Research Report
  • Research Products

    (9 results)

All 2008 2007 2006

All Journal Article (8 results) (of which Peer Reviewed: 3 results) Presentation (1 results)

  • [Journal Article] Sequential Palladiurn-catalyzed Coupling Reactions on Solid-phase2008

    • Author(s)
      Takayuki Doi
    • Journal Title

      J. Comb. Chem. 10(1)

      Pages: 135-141

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Doscovery and Combinatorial Synthesis of Fungal Metabolites Beauveriolides, Novel Antiatherosclerotiic Agents2008

    • Author(s)
      Hiroshi Tomoda
    • Journal Title

      Acc. Chern. Res. 41(1)

      Pages: 32-39

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of Dimethyl Gloiosiphone A by Way of Palladium-catalyzed Domino Cycylization2007

    • Author(s)
      Takayuki Doi
    • Journal Title

      J. Org. Chem. 72(1)

      Pages: 3667-3671

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Total Synthesis of (R)-Telomestatin2006

    • Author(s)
      Takayuki Doi
    • Journal Title

      Organic Letters 8(18)

      Pages: 4165-4167

    • Related Report
      2006 Annual Research Report
  • [Journal Article] Absolute Stereochemistry of Fungal Beauveriolide III and ACAT Inhibitory Activity of Four Stereoisomers2006

    • Author(s)
      Taichi Oshiro
    • Journal Title

      J. Org. Chem. 71(20)

      Pages: 7643-7649

    • Related Report
      2006 Annual Research Report
  • [Journal Article] Design and Synthesis of Telomestatin Derivatives and Their Inhibitory Activity of Telomerase2006

    • Author(s)
      Masayuki Tera
    • Journal Title

      Heterocycles 69

      Pages: 505-514

    • Related Report
      2006 Annual Research Report
  • [Journal Article] A Total Synthesis of Spiruchostatin A2006

    • Author(s)
      Takayuki Doi
    • Journal Title

      Tetrahedron Lett. 47(7)

      Pages: 1177-1180

    • NAID

      10020528667

    • Related Report
      2006 Annual Research Report
  • [Journal Article] Synthesis and Biological Evaluation of a Beauveriolide Analogue Library2006

    • Author(s)
      Kenichiro Nagai
    • Journal Title

      J. Comb. Chem. 8(1)

      Pages: 103-109

    • Related Report
      2006 Annual Research Report
  • [Presentation] (R)-および(S)-テロメスタチンの全合成2007

    • Author(s)
      柴田 和朗
    • Organizer
      有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      横浜国立大学常盤台キャンパス教育文化ホール
    • Year and Date
      2007-05-11
    • Related Report
      2007 Annual Research Report

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Published: 2006-04-01   Modified: 2018-03-28  

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