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Development of novel class of Cdc25A inhibitor by combination of hydrophilic and hydrophobic group

Research Project

Project/Area Number 20590110
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionTohoku University

Principal Investigator

SHIMAZAWA Rumiko  Tohoku University, 大学院・医歯薬学総合研究科, 准教授 (00411083)

Co-Investigator(Kenkyū-buntansha) KURIYAMA Masami  長崎大学, 大学院・医歯薬学総合研究科, 准教授 (40411087)
Project Period (FY) 2008 – 2010
Project Status Completed (Fiscal Year 2010)
Budget Amount *help
¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000)
Fiscal Year 2010: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2009: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2008: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Keywords脱リン酸化酵素 / Cdc25A / 複素環 / 付加反応 / 触媒的付加 / フタライド
Research Abstract

Novel N-heterocyclic derivatives were designed and synthesized as a Cdc25A inhibitor. The N-heterocyclic derivatives which have long alkyl chains exhibited strong inhibitory activity toward dual-specificity phosphatase Cdc25A. In addition, efficient synthesis of 3-arylphthalides via palladium-catalyzed 1,2-addition with the novel thioether-imidazolinium carbene ligands was successfully achieved.

Report

(4 results)
  • 2010 Annual Research Report   Final Research Report ( PDF )
  • 2009 Annual Research Report
  • 2008 Annual Research Report
  • Research Products

    (21 results)

All 2010 2009 2008

All Journal Article (8 results) (of which Peer Reviewed: 8 results) Presentation (13 results)

  • [Journal Article] Palladium-Imidazolinium Carbene-Catalyzed Arylation of Aldehydes with Arylboronic Acids in Water2010

    • Author(s)
      Kuriyama, M.; Ishiyama, N.; Shimazawa, R.; Onomura, O.
    • Journal Title

      Tetrahedron 66(34)

      Pages: 6814-6819

    • NAID

      120006984284

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Palladium-Imidazolinium Carbene-Catalyzed Arylation of Aldehydes with Arylboronic Acids in Water2010

    • Author(s)
      Kuriyama, M.; Ishiyama, N.; Shimazawa, R.; Onomura, O.
    • Journal Title

      Tetrahedron

      Volume: 66 Pages: 6814-6819

    • NAID

      120006984284

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Efficient Synthesis of 3-Arylphthalides using Palladium-Catalyzed Arylation of Aldehydes with Organoboronic Acids2009

    • Author(s)
      Kuriyama, M.; Ishiyama, N.; Shimazawa, R.; Shirai, R.; Onomura, O.
    • Journal Title

      J. Org. Chem. 74(23)

      Pages: 9210-9213

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Efficient Synthesis of 3-Arylphthalides using Palladium-Catalyzed Arylation of Aldehydes with Organoboronic Acids2009

    • Author(s)
      栗山正巳, 石山夏希, 嶋澤るみ子, 白井隆一, 尾野村治
    • Journal Title

      Journal of Organic Chemistry 74

      Pages: 9210-9213

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Palladium-Catalyzed 1,2-Addition of Potassium Aryl- and Alkenyltrifluoroborates to Aldehydes using Thioether-Imidazolinium Carbene Ligands2008

    • Author(s)
      Kuriyama, M.; Shimazawa, R.; Enomoto, T.; Shirai, R.
    • Journal Title

      J. Org. Chem. 73(17)

      Pages: 6939-6942

    • NAID

      130006998727

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of N-alkyl oxindolylidene acetic acids as a new class of potent Cdc25A inhibittors2008

    • Author(s)
      Shimazawa, R.; Kuriyama, M.; Shirai, R.
    • Journal Title

      Bioorg. Med. Chem. Lett. 18(11)

      Pages: 3350-3353

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Design and synthesis of N-alkyl oxindolylidene acetic acids as a new class of potent Cdc25A inhibitors2008

    • Author(s)
      嶋澤るみ子、栗山正巳、白井隆一
    • Journal Title

      Bioorganic and Medicinal Chemistry Letters 18

      Pages: 3350-3353

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Palladium-Catalyzed 1, 2-Addition of Potassium Aryl- and Alkeny Itrifluoroboiates to Aldehydes using Thioether-Imidazolinium Car bene Ligands2008

    • Author(s)
      栗山正巳、嶋澤るみ子、榎本光伯、白井隆一
    • Journal Title

      Journal of Organic Chemistry 73

      Pages: 6939-6942

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed
  • [Presentation] Palladium-Imidazolinium Carbene-Catalyzed Arylation of Aldehydes with Arylboronic Acids in Water2010

    • Author(s)
      Kuriyama M.; Ishiyama N.; Shimazawa R.; Onomura O.
    • Organizer
      2010 International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii, USA
    • Related Report
      2010 Final Research Report
  • [Presentation] Palladium-Imidazolinium Carbene-Catalyzed Arylation of Aldehydes with Arylboronic Acids in Water2010

    • Author(s)
      Kuriyama, M.; Ishiyama, N.; Shimazawa, R.; Onomura, O.
    • Organizer
      International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii, USA
    • Related Report
      2010 Annual Research Report
  • [Presentation] C-S二座型配位子の開発と遷移金属触媒反応への適用2009

    • Author(s)
      栗山正巳
    • Organizer
      有機合成化学協会九州山口支部 有機合成化学講演会
    • Place of Presentation
      長崎
    • Year and Date
      2009-11-20
    • Related Report
      2010 Final Research Report
  • [Presentation] Efficient Synthesis of Phthalides using Arylation of Aldehydes with Organoboronic Acids Catalyzed by Palladium/Thioether-Imidazolinium Chloride System2009

    • Author(s)
      栗山正巳, 石山夏希, 嶋澤るみ子, 白井隆一, 尾野村治
    • Organizer
      The 11^<th> International Kyoto Conferece on New Aspects of Organic Chemistry
    • Place of Presentation
      リーガロイヤルホテル(京都)
    • Year and Date
      2009-11-11
    • Related Report
      2009 Annual Research Report
  • [Presentation] 含窒素複素環カルベンを基盤とするC-S二座型配位子を用いたパラジウム触媒による有機ホウ素試薬の付加反応と応用2009

    • Author(s)
      栗山正巳, 石山夏希, 榎本光伯, 嶋澤るみ子, 白井隆一, 尾野村治
    • Organizer
      第7回次世代を担う有機化学シンポジウム
    • Place of Presentation
      大阪大学(大阪)
    • Year and Date
      2009-07-24
    • Related Report
      2009 Annual Research Report
  • [Presentation] C-S二座型配位子-パラジウム錯体を用いたアルデヒドの触媒的アリール化反応2009

    • Author(s)
      栗山正巳
    • Organizer
      第3回万有若手交流合宿セミナー
    • Place of Presentation
      唐津
    • Related Report
      2010 Final Research Report
  • [Presentation] Efficient Synthesis of Phthalides using Arylation of Aldehydes with Organoboronic Acids Catalyzed by Palladium/Thioether-Imidazolinium Chloride System2009

    • Author(s)
      Kuriyama M.; Ishiyama N.; Shimazawa R.; Shirai R.; Onomura O.
    • Organizer
      The 11^<th> International Kyoto Conferece on New Aspects of Organic Chemistry
    • Place of Presentation
      Kyoto, Japan
    • Related Report
      2010 Final Research Report
  • [Presentation] 含窒素複素環カルベンを基盤とするC-S二座型配位子を用いたパラジウム触媒による有機ホウ素試薬の付加反応と応用2009

    • Author(s)
      栗山正巳, 石山夏希, 榎本光伯, 嶋澤るみ子, 白井隆一, 尾野村治
    • Organizer
      第7回次世代を担う有機化学シンポジウム
    • Place of Presentation
      大阪
    • Related Report
      2010 Final Research Report
  • [Presentation] C-S二座配位子-パラジウム触媒を用いた有機三フッ化ホウ素塩のアルデヒドへの付加反応2008

    • Author(s)
      栗山正巳、嶋澤るみ子、榎本光伯、白井隆一
    • Organizer
      第34回反応と合成の進歩シンポジウム
    • Place of Presentation
      京都
    • Year and Date
      2008-11-04
    • Related Report
      2008 Annual Research Report
  • [Presentation] C-S二座配位子-パラジウム触媒を用いた有機三フッ化ホウ素塩のアルデヒドへの付加反応2008

    • Author(s)
      栗山正巳, 嶋澤るみ子, 榎本光伯, 白井隆一
    • Organizer
      第58回日本薬学会近畿支部大会
    • Place of Presentation
      神戸
    • Year and Date
      2008-10-25
    • Related Report
      2010 Final Research Report
  • [Presentation] C-S二座配位子-パラジウム触媒を用いた有機三フッ化ホウ素塩のアルデヒドへの付加反応2008

    • Author(s)
      栗山正巳、嶋澤るみ子、榎本光伯、白井隆一
    • Organizer
      第58回日本薬学会近畿支部総会・大会
    • Place of Presentation
      神戸
    • Year and Date
      2008-10-25
    • Related Report
      2008 Annual Research Report
  • [Presentation] C-S二座配位子-パラジウム触媒を用いた有機三フッ化ホウ素塩のアルデヒドへの付加反応2008

    • Author(s)
      栗山正巳, 嶋澤るみ子, 榎本光伯, 白井隆一
    • Organizer
      第34回反応と合成の進歩シンポジウム
    • Related Report
      2010 Final Research Report
  • [Presentation] Efficient 1,2-Addition of Organoboronic Acids to Aldehydes Catalyzed by the Palladium/Thioether-Imidazolinium Chloride System2008

    • Author(s)
      Kuriyama M.; Shimazawa R.; Shirai R.
    • Organizer
      The Fifth International Symposium on Integrated Synthesis
    • Place of Presentation
      Kobe, Japan
    • Related Report
      2010 Final Research Report

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Published: 2008-04-01   Modified: 2016-04-21  

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