Dicarba-closo-dodecaboranes as a Pharmacophore. Retinoidal Antagonists and Potential Agonists

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概要

• 論文の詳細を見る

• Synthesis and biological evaluation of the first dicarba-closo-dodecaborane (carborane) derivatives of retinoids are described. Their retinoidal activity were examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for retinoic acid receptor (RAR)) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. The 4-carboranyl-substituted compounds (7,11) showed antagonistic activity but no agonistic activity even in the presence of the potent synergist HX630. On the other hand, the 3-carboranyl-substituted compounds (8,12) showed potential agonistic activity, but no antagonistic activity. The results indicates that carboranes are applicable as the hydrophobic moiety of biologically active molecules.

• 社団法人日本薬学会の論文
• 1999-03-15

著者

• 遠藤 泰之

  東北薬科大学薬学部

• KAGECHIKA Hiroyuki

  Graduate School of Pharmaceutical Sciences, The University of Tokyo

• Kagechika Hiroyuki

  Graduate School Of Pharmaceutical Sciences The University Of Tokyo:research Foundation Itsuu Laborat

• Kagechika Hiroyuki

  Graduate School Of Biomedical Sci. Tokyo Medical And Dental Univ.

• Shudo Koichi

  Graduate School Of Pharmaceutical Sciences The University Of Tokyo

• ENDO Yasuyuki

  Graduate School of Pharmaceutical Sciences, The University of Tokyo

• TSUJI Motonori

  Graduate School of Pharmaceutical Sciences, University of Tokyo

• IIJIMA Toru

  Graduate School of Pharmaceutical Sciences, University of Tokyo

• KAWACHI Emiko

  Graduate School of Pharmaceutical Sciences, University of Tokyo

• Shudo K

  Research Foundation Itsuu Laboratory

• Kobayashi Hisayoshi

  Institute Of Molecular And Cellular Biosciences University Of Tokyo

• Iijima T

  Tohoku Pharmaceutical Universety

• Tsuji M

  Univ. Tokyo Tokyo Jpn

• Tsuji Motonori

  Graduate School Of Pharmaceutical Sciences University Of Tokyo

• Kagechika H

  Tokyo Medical And Dental Univ. Tokyo Jpn

• Ishizuka T

  Tohoku Pharmaceutical University

• Endo Yasuyuki

  Graduate School Of Pharmaceutical Sciences University Of Tokyo

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