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2012 Fiscal Year Final Research Report

Multi-functionality and structure development of thalidomide

Research Project

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Project/Area Number 21790107
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Drug development chemistry
Research InstitutionThe University of Tokyo

Principal Investigator

YACHIDE Tomomi  東京大学, 分子細胞生物学研究所, 技術職員 (20401284)

Project Period (FY) 2009 – 2012
Keywordsケミカルバイオロジー
Research Abstract

I investigated the molecular mechanism of action of thalidomide andits metabolites, and cell signaling of biologically active derivatives of thalidomide. In addition, some biologically active compounds, such as nuclear receptor agonists/antagonists and enzyme inhibitors, have been created by structural development ofthalidomide and its derivatives. Based on these studies, I proved that thalidomide is usefulas a novel multi-template for development of various kinds of biologically activecompounds.

  • Research Products

    (34 results)

All 2013 2012 2011 2010 2009 Other

All Journal Article (12 results) (of which Peer Reviewed: 12 results) Presentation (21 results) Remarks (1 results)

  • [Journal Article] Sructure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with2013

    • Author(s)
      Noguchi- Yachide, Yuichi Hashimoto and Minoru Ishikawa
    • Journal Title

      Bioorg. Med. Chem

      Volume: 21 Pages: 993-1005

    • Peer Reviewed
  • [Journal Article] Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton2013

    • Author(s)
      Yusuke Mita, Tomomi Noguchi- Yachide, Minoru Ishikawa and Yuichi Hashimoto
    • Journal Title

      Bioorg. Med. Chem

      Volume: 21 Pages: 608-617

    • Peer Reviewed
  • [Journal Article] Specific Inhibitors of Puromycin-Sensitive Aminopeptidase with a 3-(Halogenated Phenyl)-2,4(1H,3H)-quinazolinedione Skeleton.2012

    • Author(s)
      Yotaro Matsumoto, Tomomi Noguchi- Yachide, Masaharu Nakamura, Yusuke Mita, Akiyoshi Numadate, and Yuichi Hashimoto.
    • Journal Title

      Heterocycles

      Volume: 86 Pages: 1449-1463

    • Peer Reviewed
  • [Journal Article] Small-molecular inhibitors of Ca2+-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene.2012

    • Author(s)
      Shunpei Murasawa, Katsuya Iuchi, Shinichi Sato, Tomomi Noguchi- Yachide, Mikiko Sodeoka, Tsutomu Yokomatsu, Kosuke Dodo, Yuichi Hashimoto, Y. and Hiroshi Aoyama
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 20 Pages: 6384-6393

    • Peer Reviewed
  • [Journal Article] Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6 Hdibenz[b,e]azepin-6-one skeleton.2012

    • Author(s)
      Atsushi Aoyama, Kaori Endo-Umeda, Kenji Kishida, Kenji Ohgane, Tomomi Noguchi- Yachide, Hiroshi Aoyama, Minoru Ishikawa, Hiroyuki Miyachi, Makoto Makishima and Yuichi Hashimoto
    • Journal Title

      J. Med. Chem

      Volume: 55 Pages: 7360-7377

    • Peer Reviewed
  • [Journal Article] Estrogen receptor α/β ligands derived from thalidomide.2011

    • Author(s)
      Tomomi Noguchi - Yachi de, Kazuyuki Sugita and Yuichi Hashimoto.
    • Journal Title

      Heterocycles

      Volume: 83 (9) Pages: 2137-2147

    • Peer Reviewed
  • [Journal Article] Further Application of the Multi-Templ ate Approach f or Creati on of Biological Response Modifiers: Discovery of a New Class of Multifunctional Anti-Diabetic Agents.2011

    • Author(s)
      Kazunori Motoshima, Tomomi Noguchi- Yachi de, Minoru Ishikawa, Yui chi Hashi moto, and Kazuyuki Sugita
    • Journal Title

      Heterocycles

      Volume: 82 (2) Pages: 1083-1101

    • Peer Reviewed
  • [Journal Article] Novel Selective Anti-androgens with a Diphenylpentane Skeleton2010

    • Author(s)
      Keisuke Maruyama, Tomomi Noguchi- Yachi de, Kazuyuki Sugita, Yui chi Hashi moto and Mi noru Ishikawa
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 20 Pages: 6661-6666

    • Peer Reviewed
  • [Journal Article] LXXLL peptide mimetics as inhibitorsof the interaction of vitamin D receptorwith coactivators2010

    • Author(s)
      Noguchi- Yachi de, Hiroyuki Miyachi, Makoto Makishima, Yuichi Hashimoto and Minoru Ishikawa
    • Journal Title

      Bioorg. Med. Chem. Lett.

      Volume: 20 Pages: 1712-1717

    • Peer Reviewed
  • [Journal Article] b-Naphthoflavone analogs as potentand soluble aryl hydrocarbon receptoragonists: Improvement of solubility bydisruption of molecular planarity2010

    • Author(s)
      Yuj i Fuj i ta, Mi tsuhi ro Yonehara, Masashi Tetsuhashi, Tomomi Noguchi- Yachi de, Yuichi Hashimotoand Minoru Ishikawa
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 18 Pages: 1194-1203

    • Peer Reviewed
  • [Journal Article] Separation of α-glucosidase-inhibitoryand liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXR-selective antagonists.2009

    • Author(s)
      Kazunori Motoshima, Tomomi Noguchi- Yachide, Kazuyuki Sugita,Yuichi Hashimoto and Minoru Ishikawa.
    • Journal Title

      Bioorg. Med. Chem.

      Volume: 17 Pages: 5001-5014

    • Peer Reviewed
  • [Journal Article] Enhancement of Chemically-induced HL-60 Cell Differentiation by 3,3'-Diindolylmethane (DIM) Derivatives.2009

    • Author(s)
      Tomomi Noguchi - Yachi de, Masashi Tetsuhashi , Hi roshi Aoyama and Yui chi Hashimoto.
    • Journal Title

      Chem. Pharm. Bull.

      Volume: 57(5) Pages: 536-540

    • Peer Reviewed
  • [Presentation] サリドマイド由来エストロゲン受容体リガンドの創製2012

    • Author(s)
      谷内出友美、松本洋太郎、杉田和幸、橋本祐一
    • Organizer
      日本薬学会132年会
    • Place of Presentation
      北海道札幌市
    • Year and Date
      20120328-31
  • [Presentation] LiverXReceptor(LXR)リガンドの構造展開によるTransrepression作用選択的リガンドの創製2012

    • Author(s)
      青山惇、梅田(遠藤)香織、谷内出(野口)友美、石川稔、宮地弘幸、槇島誠、橋本祐一
    • Organizer
      日本薬学会132年会
    • Place of Presentation
      北海道札幌市
    • Year and Date
      20120328-31
  • [Presentation] 虚血性細胞死抑制活性を有する低分子化合物の創製2012

    • Author(s)
      村澤慎平、青山洋史、どど孝介、谷内出友美、橋本祐一
    • Organizer
      日本薬学会132年会
    • Place of Presentation
      北海道札幌市
    • Year and Date
      20120328-31
  • [Presentation] LXXLL配列を模倣したVDR-コアクチベーター相互作用阻害物質の構造活性相関2012

    • Author(s)
      三田裕介、どど孝介、谷内出友美、橋本祐一、石川稔
    • Organizer
      日本薬学会132年会
    • Place of Presentation
      北海道札幌市
    • Year and Date
      20120328-31
  • [Presentation] 免疫調節作用選択的な肝臓X受容体(LXR)リガンドの創製2012

    • Author(s)
      青山惇、梅田(遠藤)香織、岸田健治、大金賢司、谷内出(野口)友美、青山洋史、石川稔、宮地弘幸、槇島誠、橋本祐一
    • Organizer
      日本レチノイド研究会第23回学術集会
    • Place of Presentation
      鳥取県米子市
    • Year and Date
      2012-10-19
  • [Presentation] Improvement in aqueous solubility of biocyclic molecules by disruption of molecular planarity and symmetry2011

    • Author(s)
      M. Ishikawa, Y. Fujita, J. Kasuga, M. Yonehara, T. Noguchi - Ychide, H. Miyachi and Y. Hashimoto
    • Organizer
      AIMECS11, 8th AFMC International Medicinal Chemistry Symposium "Frontier of Medicinal Science"
    • Place of Presentation
      Tokyo
    • Year and Date
      20111129-1202
  • [Presentation] LXXLL peptide mimetics as inhibitors ofthe interaction of vitamin D receptor2011

    • Author(s)
      Y. Mita, K. Dodo, T. Noguchi- Yachide, H. Miyachi and Y. Hashimoto.
    • Organizer
      AIMECS11, 8th AFMC International Medicinal Chemistry Symposium "Frontier of Medicinal Science"
    • Place of Presentation
      Tokyo
    • Year and Date
      20111129-1202
  • [Presentation] Further application of the multi-template approach for creation of biologically active compounds: discovery of a new class of multifunctional anti-diabetic agents.2011

    • Author(s)
      K. Sugita, K. Motoshima, T. Noguchi- Yachide, M. Ishikawa and Y. Hashimoto.
    • Organizer
      AIMECS11, 8th AFMC International Medicinal Chemistry Symposium "Frontier of Medicinal Science"
    • Place of Presentation
      Tokyo
    • Year and Date
      20111129-1202
  • [Presentation] LXR依存的なTransrepression作用選択的リガンドの創製2011

    • Author(s)
      青山惇、遠藤香織、谷内出友美、青山洋史、石川稔、槇島誠、宮地弘幸、橋本祐一
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      20110328-31
  • [Presentation] ジフェニルペンタン骨格を有する選択的抗アンドロゲン物質の創製研究2011

    • Author(s)
      丸山慶輔、谷内出友美、杉田和幸、橋本祐一、石川稔
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      20110328-31
  • [Presentation] Design, synthesis and evaluation of transrepression-selective ligands, bearing anti-inflammatory activity mediated by LXR.2010

    • Author(s)
      A. Aoyama, T. Yachi de, H. Aoyama, M. Ishikawa, M. Makishima, H. Miyachi and Y. Hashimoto
    • Organizer
      The International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii
    • Year and Date
      20101215-20
  • [Presentation] ss-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: Improvement of solubility by disruption of molecular planarity.2010

    • Author(s)
      Y. Fuj i t a, M. Yonehara, M. Tetsuhashi, T. Noguchi - Yachi de, Y. Hashimoto and M. Ishikawa
    • Organizer
      The International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii
    • Year and Date
      20101215-20
  • [Presentation] Selective anti-androgens with a 3,3-diphenylpentane skeleton .2010

    • Author(s)
      K. Maruyama, M. Ishikawa, T. Noguchi- Yachi de and Y. Hashimoto
    • Organizer
      The International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii
    • Year and Date
      20101215-20
  • [Presentation] LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.2010

    • Author(s)
      Yachi de, H. Miyachi, Y. Hashimoto and M. Ishikawa
    • Organizer
      The International Chemical Congress of Pacific Basin Societies
    • Place of Presentation
      Hawaii
    • Year and Date
      20101215-20
  • [Presentation] 難溶性を改善したAhRリガンドの創製2010

    • Author(s)
      藤田優史、米原光拡、鉄橋正士、谷内出友美、橋本祐一、石川稔
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都テレサ
    • Year and Date
      20101117-19
  • [Presentation] LXXLL配列を模倣したビタミンD受容体-コアクチベーター相互作用阻害物質の創製-2010

    • Author(s)
      三田裕介、どど孝介、谷内出友美、宮地弘幸、橋本祐一、石川稔
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都テレサ
    • Year and Date
      20101117-19
  • [Presentation] LXRを介した抗炎症作用を有する選択的リガンドの創製2010

    • Author(s)
      青山惇、谷内出友美、青山洋史、石川稔、槇島誠、宮地弘幸、橋本祐一
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Year and Date
      20100328-30
  • [Presentation] LXXLL配列を模倣した核内受容体-コアクチベーター阻害物質の創製2010

    • Author(s)
      三田裕介、どど孝介、谷内出友美、宮地弘幸、橋本祐一、石川稔
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Year and Date
      20100328-30
  • [Presentation] 難溶性を改善したAhRリガンドの創製2010

    • Author(s)
      藤田優史、米原光拡、鉄橋正士、谷内出友美、橋本祐一、石川稔
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Year and Date
      20100328-30
  • [Presentation] 環状イミドを有するヒダントイン類の合成と活性評価2009

    • Author(s)
      山口淳一、谷内出友美、坂口由佳、柴田千秋、橋本祐一
    • Organizer
      第28回メディシナルケミストリーシンポジウム
    • Place of Presentation
      東京大学
    • Year and Date
      20091125-27
  • [Presentation] サリドマイド誘導体におけるα-glucosidaseとLXR活性の作用分離、およびglycogenphosphorylase阻害活性2009

    • Author(s)
      島和典、石川稔、谷内出友美、杉田和幸、橋本祐一
    • Organizer
      第28回メディシナルケミストリーシンポジウム
    • Place of Presentation
      東京大学
    • Year and Date
      20091125-27
  • [Remarks]

    • URL

      http://www.iam.u-tokyo.ac.jp/chem/IMCB-8ken-HP/Index.html

URL: 

Published: 2014-08-29  

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