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2007 Fiscal Year Final Research Report Summary

Development and Application of Novel 3-Dimensional Hydrophobic Structures for Drug Design, Which Are Focused on Molecular Recognition between Ligand and Receptor

Research Project

Project/Area Number 16390032
Research Category

Grant-in-Aid for Scientific Research (B)

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

Principal Investigator

ENDO Yasuyuki  Tohoku Pharmaceutical University, Faculty of Pharmaceutical Sciences, Professor (80126002)

Co-Investigator(Kenkyū-buntansha) INOMATA Kohei  Tohoku Pharmaceutical University, Faculty of Pharmaceutical Sciences, Lecturer (60221785)
OHTA Kiminori  Tohoku Pharmaceutical University, Faculty of Pharmaceutical Sciences, Assistant Professor (90347906)
Project Period (FY) 2004 – 2007
Keywordsmedicinal drug design / nuclear receptor / estrogen receptor / androgen receptor / hydrophobic interaction / antagonist / boron cluster / molecular recognition
Research Abstract

Carboranes (dicarba-closo-dodecaboranes) are a class of carbon-containing polyhedral boron-cluster compounds having globular shape, remarkable thermal stability and hydrophobic character. In this study, we applied their molecular shape and hydrophobic surface of the molecules to design and synthesis of nuclear receptor ligands. Hydrophobic and hydrogen bonding interaction of carborane derivatives, and synthetic methods of carborane derivatives for analysis and preparation of various carborane-containing compounds were also investigated. The results were summarized as follows.
1. Candidate estrogen receptor ligands with two phenolic residues on a 3-dimensional hydrophobic core structure (carborane, bicyclo[2, 2, 2]octane, adamantane) were synthesized and biologically evaluated. Amog the carborane-containing compounds, a dynamic change of agonist/antagonist balance was observed depending on the direction and the distance of the two phenolic groups.
2. Candidate androgen receptor ligands bearing carborane as a hydrophobic pharmacophore were designed based on testosterone and aromatic anti-estrogen agents, and synthesized, biologically evaluated. Novel potent non-steroidal androgen antagonists BA321, BA341 were found.
3. Intramolecular hydrogen bonding on 2-(2-hydroxyphenyl)-o-carborane and 2-(2-hydroxyphenyl)-p-carborane were observed on H-NMR study. The intranolecular hydrogen bonding was confirmed by X-ray, IR and DFT calculation.
4. A few synthetic method of carborane derivatives, such as regioselective iodination reaction on the carborane cage, facile hydroxylation of a carbon on, the carborane cage were developed.

  • Research Products

    (114 results)

All 2008 2007 2006 2005 2004 Other

All Journal Article (46 results) (of which Peer Reviewed: 24 results) Presentation (67 results) Remarks (1 results)

  • [Journal Article] Symmetric Bent-core Mesogens with m-Carborane and Adamantane As the Central Units2008

    • Author(s)
      Pociecha, D
    • Journal Title

      J.Mater.Chem (In press)

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Identification of an Intermediate in the Deboronation of ortho-Carborane:an Adduct of ortho-Carborane with Two Mucleophiles on One Boron Atom2008

    • Author(s)
      Yoshiyuki Taoda
    • Journal Title

      Chem.Commun

      Pages: 2049-2051

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Symmetric Bent-core Mesogens with m-Carborane and Adamantane As the Central Units2008

    • Author(s)
      Pociecha, D., Ohta, K., Januszko, A., Kaszynski, P.*, Endo, Y
    • Journal Title

      J. Mater. Chem (in press)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Identification of an Intermediate in the Deboronation of ortho-Carborane : an Adduct of ortho-Carborane with Two Mucleophiles on One Boron Atom2008

    • Author(s)
      Taoda, Y., Sawabe, T., Endo, Y.*, Yamaguchi, K., Fujii, S., Kagechika, H.*
    • Journal Title

      Chem. Commun

      Pages: 2049-2051

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Facile and Efficient Synthesis of C-Hydroxycarboranes and C,C'-Dihydroxycarboranes2007

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Inorg.Chem 46

      Pages: 3966-3970

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Solid-state Supramolecular Array through Cooperative,p-p Interactions of 1-(2-Methoxyphenyl)-o-carborane2007

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Tetrahedron 63

      Pages: 12160-12165

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] ホウ素クラスター:カルボランの有機化学-合成、構造、立体分子構築への応用2007

    • Author(s)
      遠藤 泰之
    • Journal Title

      有機合成化学協会誌 65

      Pages: 320-333

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Facile and Efficient Synthesis of C-Hydroxycarboranes and C, C'-Dihydroxycarboranes2007

    • Author(s)
      Ohta, K., Goto, T., Yamazaki, H., Pichierri, F. : Endo, Y.*
    • Journal Title

      Inorg. Chem 46

      Pages: 3966-3970

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Proton-Driven Conformational Change in a 2-Aryl-p-carborane Constrained by an Intramolecular C-H-O Hydrogen Bond2007

    • Author(s)
      K. Ohta, K., Yamazaki, H., Kawahata, M., Yamaguchi, K., Pichierri, F., Endo. Y.*
    • Journal Title

      Tetrahedron. Lett 48

      Pages: 5231-5234

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Solid-state Supramolecular Array through Cooperative tt-it Interactions of -(2-Methoxyphenyl)-o-carborane2007

    • Author(s)
      Ohta, K., Yamazaki, H., Pichierri, F., Kawahata, M., Yamaguchi, K., Endo, Y.*
    • Journal Title

      Tetrahedron 63

      Pages: 12160-12165

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] NMR Study of 1,2-Dicarba-closo-dodecaboranes: Intramolecular C-H-O Hydrogen Bonding in Solution2006

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Tetrahedron.Lett 47

      Pages: 1937-1940

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] m-Carborane Bisphenol Structure as a Pharmacophore for Selective Estrogen Receptor Modulators2006

    • Author(s)
      Takumi Ogawa
    • Journal Title

      Bioorg.Med.Chem.Lett 16

      Pages: 3943-3946

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Genetic and Pharmacological Evidence that a Retinoic Acid Cannot be the RXR-activating Ligand in Mouse Epidermis Keratinocytes2006

    • Author(s)
      Calleja, C
    • Journal Title

      Genes Dev 20

      Pages: 1525-1538

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Masogenic,Optical and Dielectric Properties of 5-Substituted 2-[12-(4-pentyloxy phenyl)-p- carboran-l-yl][1,3]dioxanes2006

    • Author(s)
      Takashi Nagamine
    • Journal Title

      J.Mater.Chem 6

      Pages: 3836-3843

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] 創薬化学における新規3次元的疎水性構造単位の開発と応用2006

    • Author(s)
      遠藤 泰之
    • Journal Title

      ファルマシア 42

      Pages: 421-425

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] m-Carborane Bisphenol Structure as a Pharmacophore for Selective Estrogen Receptor Modulators2006

    • Author(s)
      Ogawa, T., Ohta K, Yoshimi, T., Yamazaki, H., Suzuki, T., Ohta, S., Endo, Y.*
    • Journal Title

      Bioorg. Med. Chem. Lett 16

      Pages: 3943-3946

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Genetic and Pharmacological Evidence that a Retinoic Acid Cannot be the RXR-activating Ligand in Mouse Epidermis Keratinocytes2006

    • Author(s)
      Calleja, C., Messaddeq, N., Chapellier, B., Yang, H., Krezel, W., Li, M., Metzger, D., Marcrez, B., Ohta, K., kagechika H, Endo, Y., Mark, M., Ghyselinck, N. B., Chambon, P.*
    • Journal Title

      Genes Dev 20

      Pages: 1525-1538

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Ohta, K., . Endo. Y. Masogenic, Optical and Dielectric Properties of 5-Substituted 2-[12-(4-pentyloxyphenyl) p- carboran-l-yl][1, 3]dioxanes2006

    • Author(s)
      Nagamine, T., Januszko, A., Kaszynski, P.*
    • Journal Title

      I. Mater. Chem 6

      Pages: 3836-3843

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] A new Class of Androgen Receptor Antagonists Bearing Carborane in Place of a Steroidal Skeleton2005

    • Author(s)
      Shinya Fujii
    • Journal Title

      BioMed Chem.Lett 46

      Pages: 227-230

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] New Synthetic Method of 1,2-Diaryl-l,2-dicarba-closo-dodecaboranes Employing Aromatic Nucleouhilic Substitution(SNAr) Reaction2005

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Tetrahedron Lett 46

      Pages: 483-485

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] A Distorted Benzene Bearing Two Bulky Substituents on Adjacent Positions: Structure of 1,2-Bis(1,2-Dicarba-closo-dodecaboran-l-yl)benzene2005

    • Author(s)
      Yasuyuki Endo
    • Journal Title

      Tetrahedron Lett 46

      Pages: 699-702

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Regioselective Synthesis of Triiodo-o-carboranes and Tetraiodo-o-carborane2005

    • Author(s)
      Hiroto Yamazaki
    • Journal Title

      Tetrahedron Lett 46

      Pages: 3119-3122

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Synthesis of Distorted Molecules Based on Spatial Control with Icosahedral Carboranes2005

    • Author(s)
      Yasuyuki Endo
    • Journal Title

      J.Organomet.Chem 690

      Pages: 2750-2756

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Potent Estrogen Receptor Ligands Based on Bisphenols with Globular Hydrophobic Cores2005

    • Author(s)
      Yasuyuki Endo
    • Journal Title

      J.Med.Chem 48

      Pages: 3941-3944

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Potent Androgen Antagonists Based on Carborane As a Hydrophobic Core Structure2005

    • Author(s)
      Shinya Fujii
    • Journal Title

      J.Med.Chem 48

      Pages: 4654-4662

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Design and Synthesis of Novel Androgen Receptor(AR) Antagonists with Sterically Bulky Icosahedral Carboranes2005

    • Author(s)
      Tokuhito Goto
    • Journal Title

      Bioorg.Med.Chem 13

      Pages: 6414-6424

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] A comparison of Mesogenic Properties of p-Carborane-1,12-dicarbaldehyde Schiff Bases with Their Terephthaldehyde Analogues2005

    • Author(s)
      Takashi Nagamine
    • Journal Title

      Liq.Cryst 32

      Pages: 985-995

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] 1,2-Dicarba-closo-dodecaboran-l-yl Naphthalene Derivatives2005

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Inorg.Chem 44

      Pages: 8569-8573

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] New Synthetic Method of 1, 2-Diaryl-1, 2-dicarba-closo-dodecaboranes Employing Aromatic Nucleophilic Substitution(SNAr) Reaction2005

    • Author(s)
      Ohta, K., Goto, T., Endo, Y.*
    • Journal Title

      Tetrahedron Lett 46

      Pages: 483-485

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] A Distorted Benzene Bearing Two Bulky Substituents on Adjacent Positions : Structure of 1, 2-Bis(I, 2-Dicarba-closo-dodecaboran-1-yl)benzene2005

    • Author(s)
      Endo, Y.*, Songkram, C., Ohta, K., Kaszynski, P., Yamaguchi, K
    • Journal Title

      Tetrahedron Lett 46

      Pages: 699-702

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Regioselective Synthesis of Triiodo-o-carboranes and Tetraiodo-o-carborane2005

    • Author(s)
      Yamazaki, H., Ohta, K., Endo, Y.*
    • Journal Title

      Tetrahedron Lett 46

      Pages: 3119-3122

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Synthesis of Distorted Molecules Based on Spatial Control with Icosahedral Carboranes2005

    • Author(s)
      Endo, Y.*, Songkram, C., Ohta, K., Yamaguchi, K
    • Journal Title

      J. Organomet. Chem 690

      Pages: 2750-2756

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Potent Estrogen Receptor Ligands Based on Bisphenols with Globular Hydrophobic Cores2005

    • Author(s)
      Endo, Y*., Yoshimi, T., Ohta, K., Suzuki, T., Ohta, S
    • Journal Title

      J. Med. Chem 48

      Pages: 3941-3944

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Potent Androgen Antagonists Based on Carborane As a Hydrophobic Core Structure.2005

    • Author(s)
      Fujii, S., Goto, T., Ohta, K., Hashimoto, Y., Suzuki, T., Ohta, S., Endo, Y.*
    • Journal Title

      J. Med. Chem 48

      Pages: 4654-4662

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Design and Synthesis of Novel Androgen Receptor(AR) Antagonists with Sterically Bulky Icosahedral Carboranes2005

    • Author(s)
      Goto, T., Ohta, K., Suzuki, T., Ohta, S., Endo, Y.*
    • Journal Title

      Bioorg. Med. Chem 13

      Pages: 6414-6424

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] A comparison of Mesogenic Properties of p-Carborane-1, 12-dicarbaldehyde Schiff Bases with Their Terephthaldehyde Analogues2005

    • Author(s)
      Nagamine, T., Januszko, A., Ohta, K., Kaszynski, P., Endo, Y
    • Journal Title

      Liq. Cryst 32

      Pages: 985-995

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] 1, 2-Dicarba-closo-dodecaboran-1-yl Naphthalene Derivatives2005

    • Author(s)
      Ohta, K., Goto, T., Endo, Y.*
    • Journal Title

      Inorg. Chem 44

      Pages: 8569-8573

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] NMR Study of 1, 2-Dicarba-closo-dodecaboranes : Intramolecular C-H-O Hydrogen Bonding in Solution2005

    • Author(s)
      Ohta, K., Yamazaki, H., Endo, Y.*
    • Journal Title

      Tetrahedron. Lett 47

      Pages: 1937-1940

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Structural Effects in Three-Ring Mesogenic Derivatives of p-Carborane and Their Hydrocarbon Analogs2004

    • Author(s)
      Kiminori Ohta
    • Journal Title

      ILiq.Cryst 31

      Pages: 1-12

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Novel Retinoid X Receptor(RXR) Antagonists Having a Dicarba-closododecaborane as a Hydrophobic Moiety2004

    • Author(s)
      Kiminori Ohta
    • Journal Title

      BioMed.Chem.Lett 14

      Pages: 5913-5918

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] A New Application of Inorganic Cluster,Carboranes for Medicinal Drug Design and Molecular Construction2004

    • Author(s)
      Yasuyuki Endo
    • Journal Title

      Phosphorous, Sulfur, and Silicon 179

      Pages: 799-802

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Proton-Driven Conformational Change in a 2-Aryl-p-carborane Constrained by an Intramolecular C-H-O Hydrogen Bond2004

    • Author(s)
      Kiminori Ohta
    • Journal Title

      Tetrahedron.Lett 48

      Pages: 5231-5234

    • Description
      「研究成果報告書概要(和文)」より
    • Peer Reviewed
  • [Journal Article] Structural Effects in Three-Ring Mesogenic Derivatives of p-Carborane and Their Hydrocarbon Analogs2004

    • Author(s)
      Ohta, K., Januszko, A., Kaszynski, P., Nagamine, T., Sasnouski, G., Endo, Y
    • Journal Title

      Liq. Cryst 31

      Pages: 1-12

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] Novel Retinoid X Receptor(RXR) Antagonists Having a Dicarba-closo-dodecaborane as a Hydrophobic Moiety2004

    • Author(s)
      Ohta, K., Iijima, T., Kawachi, E., Kagechika, H., Endo, Y*
    • Journal Title

      BioMed. Chem. Lett 14

      Pages: 5913-5918

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] A New Application of Inorganic Cluster, Carboranes for Medicinal Drug Design and Molecular Construction2004

    • Author(s)
      Endo, Y.*, Ohta, K., Yoshimi, T., Yamaguchi, K
    • Journal Title

      Phosphorous, Sulfur, and Silicon 179

      Pages: 799-802

    • Description
      「研究成果報告書概要(欧文)」より
  • [Journal Article] A new Class of Androgen Receptor Antagonists Bearing Carborane in Place of a Steroidal Skeleton2004

    • Author(s)
      Fujii, S., Hashimoto, Y., Suzuki, T., Ohta, S., Endo, Y*
    • Journal Title

      BioMed. Chem. Lett 15

      Pages: 227-230

    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] 性ホルモンのアゴニスト/アンタゴニストの合成と活性2008

    • Author(s)
      遠藤 泰之
    • Organizer
      東京農工大学工学部
    • Place of Presentation
      小金井
    • Year and Date
      2008-03-28
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルポラン環B-アリール化反応と機能性分子構築への応用2008

    • Author(s)
      相澤 光栄
    • Organizer
      第128回日本薬学会年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-27
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] ジフェニルアミン骨格を有するエストロゲン受容体(ER)制御化合物の構造活性相関2008

    • Author(s)
      千葉 由紀
    • Organizer
      第128回日本薬学会年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-27
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 疎水性構造上の置換基によるERα及びERβ選択性の制御2008

    • Author(s)
      小川 卓巳
    • Organizer
      第128回日本薬学会年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-27
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルボランC-H水素の相互作用を利用したホスト分子の構築2008

    • Author(s)
      山崎 広人
    • Organizer
      第128回日本薬学会年会
    • Place of Presentation
      横浜
    • Year and Date
      2008-03-26
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] シクロアルケンを疎水性構造として利用した高活性エストロゲン受容体(ER)リガンド2007

    • Author(s)
      田口 史
    • Organizer
      第127回日本薬学会年会
    • Place of Presentation
      富山
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 抗アンドロゲン活性およびエストロゲン活性を併せ持つdiarylcarborane誘導体の創製2007

    • Author(s)
      後藤 徳仁
    • Organizer
      第127回躰薬学会年会
    • Place of Presentation
      富山
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] ハロゲン原子導入による新規カルボラン含有ERβ選択的リガンド2007

    • Author(s)
      小川 卓巳
    • Organizer
      第127回日本薬学会年会
    • Place of Presentation
      富山
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 複素環官能基を水素結合部位として利用した新規ARリガンド2007

    • Author(s)
      藤井 晋也
    • Organizer
      第127回日本薬学会年会
    • Place of Presentation
      富山
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルボラノールの結晶構造と物性評価2007

    • Author(s)
      山崎 広人
    • Organizer
      日本化学会第87春季年会
    • Place of Presentation
      大阪
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 球状疎水性分子とシクロデキストリンにおける相互作用の解析2007

    • Author(s)
      遠藤 泰之
    • Organizer
      日本化学会第87春季年会
    • Place of Presentation
      大阪
    • Year and Date
      20070300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規ERβ選択的リガンドの創製:親和性の向上と選択性におけるハロゲンの効果2007

    • Author(s)
      小川 卓巳
    • Organizer
      第26回メディシナルケミストリーシンポジウム
    • Place of Presentation
      相模原
    • Year and Date
      2007-11-28
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルボランの特性を活かした多重分子標的型リガンドの創製:ERアゴニスト、ARアンタゴニストデュアルモデュレーターの開発2007

    • Author(s)
      後藤 徳仁
    • Organizer
      第26回メディシナルケミストリーシンポジウム
    • Place of Presentation
      相模原
    • Year and Date
      2007-11-28
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] アミド構造を有する含カルボランARリガンドの構造活性相関2007

    • Author(s)
      藤井 晋也
    • Organizer
      第26回メディシナルケミストリーシンポジウム
    • Place of Presentation
      相模原
    • Year and Date
      2007-11-28
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規エストロゲン受容体調節薬の創製:疎水性骨格の変換による構造活性相関2006

    • Author(s)
      田口 史
    • Organizer
      第25回メディシナルケミストリーシンポジウム
    • Place of Presentation
      名古屋
    • Year and Date
      20061100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規カルボラン含有エストロゲン受容体β選択的リガンドの創製2006

    • Author(s)
      小川 卓巳
    • Organizer
      第25回メディシナルケミストリーシンポジウム
    • Place of Presentation
      名古屋
    • Year and Date
      20061100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Diarylcarboraneを基本骨格とするアンドロゲン受容体アンタゴニストの設計と構造展開2006

    • Author(s)
      後藤 徳仁
    • Organizer
      第25回メディシナルケミストリーシンポジウム
    • Place of Presentation
      名古屋
    • Year and Date
      20061100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Design and Synthesis of Novel Androgen Receptor(AR) Modulators Focu ed on Hydrophobic Interaction2006

    • Author(s)
      Ohta, K.
    • Organizer
      The 30th.National Medicinal Chemistry Symposium
    • Place of Presentation
      Seattle,WA,US
    • Year and Date
      20060600
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Potent Estrogen Receptor Modulators Based on 3-Dimensional Hydropho bic Core Structure2006

    • Author(s)
      Endo, Y.
    • Organizer
      The 30th National Medicinal Chemistry Symposium
    • Place of Presentation
      Seattle,WA,US
    • Year and Date
      20060600
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Design and Synthesis of Novel Androgen Receptor(AR) Modulators Focued on Hydrophobic Interaction2006

    • Author(s)
      Ohta, K., Goto, T., Suzuki, T., Ohta, S
    • Organizer
      The 30th National Medicinal Chemistry Symposium
    • Place of Presentation
      Seattle, WA, US
    • Year and Date
      20060600
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Potent Estrogen Receptor Modulators Based on 3-Dimensional Hydrophobic Core Structure2006

    • Author(s)
      Endo, Y., Ogawa, T., Yoshimi, T., Ohta, K., Suzuki, T., Ohta, S
    • Organizer
      The 30th National Medicinal Chemistry Symposium
    • Place of Presentation
      Seattle, WA, US
    • Year and Date
      20060600
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Application of Inorganic Boron Cluster, Carboranes for Medicinal Drug Design2006

    • Author(s)
      Yasuyuki, Endo
    • Organizer
      Department of Chemistry, University of Washington
    • Place of Presentation
      Seattle, WA, US
    • Year and Date
      20060600
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Diphenyl-m-carboraneを基本骨格とする新規アンドロゲ学受容体(AR)アンタゴニストの創製2006

    • Author(s)
      後藤 徳仁
    • Organizer
      第126回日本薬学会年会
    • Place of Presentation
      仙台
    • Year and Date
      20060300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規エストロゲン依存性乳がん治療薬の創製研究2006

    • Author(s)
      小川 卓巳
    • Organizer
      第126回日本薬学会年会
    • Place of Presentation
      仙台
    • Year and Date
      20060300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルボランの特性を利用した溶媒環境に応答する分子スイッチの合成とその性質2006

    • Author(s)
      太田 公規
    • Organizer
      第126回日本薬学会年会
    • Place of Presentation
      仙台
    • Year and Date
      20060300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] ホウ素クラスターの特性を利用した溶液環境に応答する分子スイッチの合成とその応用2006

    • Author(s)
      山崎 広人
    • Organizer
      日本化学会第86春季年会
    • Place of Presentation
      千葉
    • Year and Date
      20060300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 球状疎水性分子とシクロデキストリンとの疎水性相互作用の解析2006

    • Author(s)
      今野 俊輔
    • Organizer
      第45回日本薬学会東北支部大会
    • Place of Presentation
      山形
    • Year and Date
      2006-10-29
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 薬物受容体の形状認識に焦点を当てた新規立体的疎水性構造単位の開発と応用2006

    • Author(s)
      遠藤 泰之
    • Organizer
      Department of Chemistry, Washington University
    • Place of Presentation
      Seattle,WA,US
    • Year and Date
      2006-06-29
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] ホウ素クラスターのC-H水素結合を利用した新規アニオンレセプターの開発2006

    • Author(s)
      山崎 広人
    • Organizer
      第1回ホスト・ゲスト化学シンポジウム
    • Place of Presentation
      つくば
    • Year and Date
      2006-05-19
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] o-カルボランの特性を利用した新規脱アルキル化反応とその応用2005

    • Author(s)
      山崎 広人
    • Organizer
      第31回反応と合成の進歩シンポジウム
    • Place of Presentation
      神戸
    • Year and Date
      20051100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規疎水性骨格を有するアンドロゲン受容体アンタゴニストの創製2005

    • Author(s)
      後藤 徳仁
    • Organizer
      第24回メディシナルケミストリーシンポジウム
    • Place of Presentation
      大阪
    • Year and Date
      20051100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 球状疎水性骨格を有する新規エストロゲン受容体リガンドの創製2005

    • Author(s)
      小川 卓巳
    • Organizer
      第44回日本薬学会東北支部大会
    • Place of Presentation
      仙台
    • Year and Date
      20051000
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 1-Aryl -1,2-dicarba-closo-dodecaboranes Evaluation of the ability of intranolecular C-H-O hydrogen bonds in solution2005

    • Author(s)
      Ohta, K
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Structure-activity study of nuclear androgen receptor(AR) antagonistd bearing carborane as a hydrophobic pharmacophore2005

    • Author(s)
      Goto, T
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] The effect of the linking group on mesogenic properties of three-ring mesegenic derivatives of p-carborane2005

    • Author(s)
      Nagamine, T.
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Design,Synthesis and biological evaluation of estrogen receptor modulators with m-carborane as a hydrophobic pharmacophore2005

    • Author(s)
      Ogawa, T.
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Regioselective iodination of o-carborane and construction of carboracycle utilyzed acidity of o-carborane C-H2005

    • Author(s)
      Yamazaki, H
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Identification of A Possible Intermediate for the Deboronation of ortho-Carborane2005

    • Author(s)
      Kagechika, H
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 1-Aryl-1, 2-dicarba-closo-dodecaboranes : Evaluation of the ability of intranolecular C-H-O hydrogen bonds in solution2005

    • Author(s)
      Ohta, K., Yamazaki, H., Endo, Y
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Structure-activity study of nuclear androgen receptor(AR) antagonistd bearing carborane as a hydrophobic pharmacophore2005

    • Author(s)
      Goto, T., Ohta, K., Endo, Y., Suzuki, T., Ohta, S
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] The effect of the linking group on mesogenic properties of three-ring mesegenic derivatives of p-carborane2005

    • Author(s)
      Nagamine, T., Ohta, K., Endo. Y., Januszko, A., Kaszynski, P
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Design, Synthesis and biological evaluation of estrogen receptor modulators with m-carborane as a hydrophobic pharmacophore2005

    • Author(s)
      Ogawa, T., Ohta, K., Endo, Y., Suzuki, T., Ohta, S
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Regioselective iodination of o-carborane and construction of carboracycle utilyzed acidity of o-carborane C-Ht2005

    • Author(s)
      Yamazaki, H., Ohta, K., Endo, Y
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Identification of A Possible Intermediate for the Deboronation of ortho-Carborane2005

    • Author(s)
      Taoda, Y., Endo, Y., Yamaguchi, K., Kagechika, H
    • Organizer
      The 12th International Conference on Boron Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20050900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Application of Inorganic Boron Cluster, Carboranes for Medicinal Drug Design2005

    • Author(s)
      Yasuyuki, Endo
    • Organizer
      Department of Chemistry, Vanderbilt University
    • Place of Presentation
      Nashville, TN, US
    • Year and Date
      20050700
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Application of Inorganic Boron Cluster, Carboranes for Medicinal Drug Design2005

    • Author(s)
      Yasuyuki, Endo
    • Organizer
      Department of Chemistry, University of Utah
    • Place of Presentation
      Salt Lake City, UT, US
    • Year and Date
      20050700
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] o-カルボランの特性に基づいた位置選択的置換基導入反応の開発と環状分子レセプターの構築2005

    • Author(s)
      山崎 広人
    • Organizer
      第125回日本薬学会年会
    • Place of Presentation
      東京
    • Year and Date
      20050300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 新規ボロキシン-アミン錯体の合成とその構造2005

    • Author(s)
      長峰 高志
    • Organizer
      第125回日本薬学会年会
    • Place of Presentation
      東京
    • Year and Date
      20050300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] カルボラン含有アンドロゲン受容体(AR)リガンドの構造活性相関2005

    • Author(s)
      後藤 徳仁
    • Organizer
      第125回日本薬学会年会
    • Place of Presentation
      東京
    • Year and Date
      20050300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 球状疎水性構造単位を利用したエストロゲン受容体調節薬の設計と合成2005

    • Author(s)
      小川 卓巳
    • Organizer
      第125回日本薬学会年会
    • Place of Presentation
      東京
    • Year and Date
      20050300
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 薬物受容体の形状認識に焦点を当てた新規立体的疎水性構造単位の開発と応用2005

    • Author(s)
      遠藤 泰之
    • Organizer
      東レ医薬研究所
    • Place of Presentation
      鎌倉
    • Year and Date
      2005-12-09
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 薬物-受容体の形状認識に焦点を当てた新規立体的疎水性構造単位の開発と応用2005

    • Author(s)
      遠藤 泰之
    • Organizer
      日本薬学会北海道支部大会 特別講演会
    • Place of Presentation
      札幌
    • Year and Date
      2005-12-03
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 受容体構造に基づく新規坑エストロゲン薬、坑アンドロゲン薬の創製2005

    • Author(s)
      遠藤 泰之
    • Organizer
      東北薬科大学生涯教育セミナー
    • Place of Presentation
      仙台
    • Year and Date
      2005-11-19
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 疎水性構造上の置換基によるERα及びERβ選択性の制御2005

    • Author(s)
      小川 卓巳
    • Organizer
      Department of Chemistry, University of Utah
    • Place of Presentation
      Salt Lake City,UT,US
    • Year and Date
      2005-07-08
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Application of Inorganic Boron Cluster,Carboranes for Medicinal Drug Design2005

    • Author(s)
      Yasuyuki Endo
    • Organizer
      Department of Chemistry, Vanderbilt University
    • Place of Presentation
      Nashville,TN,US
    • Year and Date
      2005-07-06
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 薬物受容体の形状認識に焦点を当てた新規立体的疎水性構造単位の開発と応用2005

    • Author(s)
      遠藤 泰之
    • Organizer
      東京医科歯科大学
    • Place of Presentation
      東京
    • Year and Date
      2005-03-11
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 溶液中におけるo-カルボランC-H水素と水素結合受容性基との相互作用2004

    • Author(s)
      太田 公規
    • Organizer
      第125回日本薬学会年会
    • Place of Presentation
      東京
    • Year and Date
      20041100
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] ホウ素クラスターを利用した立体分子構築2004

    • Author(s)
      山崎 広人
    • Organizer
      第43回日本薬学会東北支部大会
    • Place of Presentation
      秋田
    • Year and Date
      20041000
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] 球状疎水性構造を基本骨格とした選択的エストロゲン受容体リガンドの設計、合成と活性評価2004

    • Author(s)
      遠藤 泰之
    • Organizer
      第23回メディシナルケミストリーシンポジウム/第12回日本薬学会医薬化学部会年会
    • Place of Presentation
      つくば
    • Year and Date
      20041000
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Distorted Molecules Based on Spatial Definition of Carboranes2004

    • Author(s)
      Endo, Y.
    • Organizer
      The 3rd European Meeting on Boron Chemistry
    • Place of Presentation
      Prague,Czech Republic
    • Year and Date
      20040900
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Distorted Molecules Based on Spatial Definition of Carboranes2004

    • Author(s)
      Endo, Y., Songkram, C., Ohta, K., Yamaguchi, K
    • Organizer
      The 3rd European Meeting on Boron Chemistry
    • Place of Presentation
      Prague, Czech Republic
    • Year and Date
      20040900
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Construction of Three-dimensional Structures Based on Globular Icosahedral Carboranes and Planar Aromatic Species2004

    • Author(s)
      Endo, Y
    • Organizer
      70th Birthday Symposium for Leo Paquette
    • Place of Presentation
      Columbus, OH, US
    • Year and Date
      20040700
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] Utility of Boron Clusters for Drug Design.QSAR between Estrogen Receptor Binding Affinity and Hydrophobicity of Carboranylphenols2004

    • Author(s)
      Ohta, K
    • Organizer
      The 29th National Medicinal Chemistry Symposium
    • Place of Presentation
      Madison,WI US
    • Year and Date
      20040600
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Construction of Three-dimensional Structures Based on Globular Icosahedral Carboranes and Planar Aromatic Species2004

    • Author(s)
      Endo, Y.
    • Organizer
      70th Birthday Symposium for Leo Paquette
    • Place of Presentation
      Columbus,OH US
    • Year and Date
      20040600
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] Utility of Boron Clusters for Drug Design. QSAR between Estrogen Receptor Binding Affinity and Hydrophobicity of Carboranylphenols2004

    • Author(s)
      Ohta, K., Yamamoto, K., Endo, Y
    • Organizer
      29th National Medicinal Chemistry Symposium
    • Place of Presentation
      Madison, WI, US
    • Year and Date
      20040600
    • Description
      「研究成果報告書概要(欧文)」より
  • [Presentation] New Estrogen Receptor Modulators Bearing Carborane As A Hydrophobic Skeletal Structure2004

    • Author(s)
      Endo, Y.
    • Organizer
      The 7th French-Japanese Symposium on Medicinal and Fine Chemistry
    • Place of Presentation
      Sendai
    • Year and Date
      20040500
    • Description
      「研究成果報告書概要(和文)」より
  • [Presentation] New Estrogen Receptor Modulators Bearing Carborane As A Hydrophobic Skeletal Structure2004

    • Author(s)
      Endo Y, Yoshimi, T., Ohta, K., Miyaura, C
    • Organizer
      The 7th French-Japanese Symposium on Medicinal and Fine Chemistry
    • Place of Presentation
      Sendai, Japan
    • Year and Date
      20040500
    • Description
      「研究成果報告書概要(欧文)」より
  • [Remarks] 「研究成果報告書概要(和文)」より

    • URL

      http://www.tohoku-pharm.ac.jp/laboratory/soyaku/index.html

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Published: 2010-02-04  

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