Dicarba-closo-dodecaboranes as a Pharmacophore. Novel Potent Retinoidal Agonists
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概要
- 論文の詳細を見る
The synthesis and biological evaluation of the dicarba-closo-dodecaborane (carborane) derivatives of retinoids are described. Retinoidal activity was examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for the retinoid receptor RAR) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. 4-[4-(1,2-Dicarba-closo-dodecaboran-1-yl)phenylamino]benzoic acids and 4-[3-(1,2-dicarba-closo-dodecaboran-1-yl)phenylamino]benzoic acids showed potent agonistic activity at concentrations of 10^<-8>-10^<-9> M. The results indicate that carboranes are applicable as the hydrophobic moiety of biologically active molecules.
- 社団法人日本薬学会の論文
- 1999-04-15
著者
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遠藤 泰之
東北薬科大学薬学部
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KAGECHIKA Hiroyuki
Graduate School of Pharmaceutical Sciences, The University of Tokyo
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Kagechika Hiroyuki
Graduate School Of Pharmaceutical Sciences The University Of Tokyo:research Foundation Itsuu Laborat
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Kagechika Hiroyuki
Graduate School Of Biomedical Sci. Tokyo Medical And Dental Univ.
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Shudo Koichi
Graduate School Of Pharmaceutical Sciences The University Of Tokyo
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ENDO Yasuyuki
Graduate School of Pharmaceutical Sciences, The University of Tokyo
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IIJIMA Toru
Graduate School of Pharmaceutical Sciences, University of Tokyo
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OHTA Kiminori
Graduate School of Pharmaceutical Sciences, University of Tokyo
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KAWACHI Emiko
Graduate School of Pharmaceutical Sciences, University of Tokyo
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Shudo K
Research Foundation Itsuu Laboratory
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Kobayashi Hisayoshi
Institute Of Molecular And Cellular Biosciences University Of Tokyo
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Ohya Kumiko
Department Of Clinical Pharmacology And Toxicology Showa Pharmaceutical University
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Iijima T
Tohoku Pharmaceutical Universety
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Kagechika H
Tokyo Medical And Dental Univ. Tokyo Jpn
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Ishizuka T
Tohoku Pharmaceutical University
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Endo Yasuyuki
Graduate School Of Pharmaceutical Sciences University Of Tokyo
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