A Synthesis of 2-Substituted 2-Aminoethanol Derivatives Having Inhibitory Activity against Protein Kinase C

Tameo IWASAKI; Hiroyoshi YAMAZAKI; Takashi NISHITANI; Kazuhiko KONDO; Tadashi SATO

doi:10.1248/cpb.40.122

岩崎為雄, 山崎裕義, 西谷喬, 近藤一彦, 佐藤忠司

著者情報

キーワード: protein kinase C, aminonorbornene, 2-aminoethanol, protein kinase C inhibitor, aminonorbornane

ジャーナルフリー

1992 年 40 巻 1 号 p. 122-126

DOI https://doi.org/10.1248/cpb.40.122

詳細

抄録

A series of 2-aminoethanol derivatives was synthesized and their inhibitory activities against protein kinase C were investigated. Among these compounds, 2-endo-hexadecylamino-5-norbornene-2-exo-methanol (4h) and 2-endo-hexadecylamino-5-norbornene-2, 3-exo-dimethanol (4i) inhibited protein kinase C at the IC₅₀ values of 2×10^-5 and 1×10^-5 M, respectively, but not protein kinase A at a concentration of 1×10^-3 M. The structure-activity relationships are discussed.

責任著者(Corresponding author)

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