Tumor Necrosis Factor-Alpha Production Enhancing Activity of Substituted 3'-Methylthalidomide : Influence of Substituents at the Phthaloyl Moiety on the Activity and Stereoselectivity

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概要

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• The synthesis and tumor necrosis factor (TNF)-α production enhancing activity of substituted 3'-methyl-thalidomides on human leukemia cell line HL-60 stimulated with 12-O-tetradecanoyl-phorbol 13-acetate (TPA) are described. Though the introduction of an electron-donating amino group at the phthaloyl moiety of α-methylthalidomides enhanced the activity, substituted α-methylthalidomides showed decreased stereoselectivity as compared to that of non-substituted α-methylthalidomide. The data indicates that the TNF-α production enhancing activity of thalidomide derivatives depends on both the electronic-state of substituents at the fused benzene ring and the stereochemistry of the glutarimide moiety.

• 公益社団法人日本薬学会の論文
• 1998-07-15

著者

• 小磯 邦子

  東大分生研

• MIYACHI Hiroyuki

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

• HASHIMOTO Yuichi

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

• Hashimoto Yuichi

  Univ. Tokyo Tokyo Jpn

• LIU Jun

  Department of Physiology and Molecular Medicine, Medical College of Ohio

• KOISO Yukiko

  Institute of Molecular and Cellular Biosciences, University of Tokyo

• Hashimoto Y

  Graduate School Of Pharmaceutical Sciences Kyushu University

• SHIRAI Ryuichi

  Institute of Molecular and Cellular Biosciences, The University of Tokyo

• Miyachi Hiroyuki

  Institute Of Molecular And Cellular Biosciences The University Of Tokyo

• Hashimoto Yuichi

  Institute Of Molecular & Cellular Biosciences University Of Tokyo

• Liu Jun

  Department Of Applied Physics And Chemistry And Institute For Laser Science University Of Electro-co

• Shirai R

  Research And Education Center For Materials Science Nara Institute Of Science And Technology

• NIWAYAMA Satomi

  Departments of Biology and Chemistry, Center for Cancer Research, Massachusetts Institute of Technol

• Niwayama S

  Departments Of Biology And Chemistry Center For Cancer Research Massachusetts Institute Of Technolog

• Niwayama Satomi

  Department Of Chemistry And Biochemistry Texas Tech University

• Shirai Ryuichi

  Institute Of Molecular And Cellular Biosciences (imcb) The University Of Tokyo

• Liu Jun

  Departments Of Biology And Chemistry Center For Cancer Research Massachusetts Institute Of Technolog

• Liu Jun

  Department Of Applied Chemistry China Agricultural University

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