Structure-Activity Relationship of Novel Vitamin K Analogues as Steroid and Xenobiotic Receptor (SXR) Agonists

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  • 核内受容体SXR (Steroid and Xenobiotic Receptor) のアゴニスト活性を持つ新規ビタミンK誘導体の合成と構造活性相関の検討
  • カク ナイ ジュヨウタイ SXR(Steroid and Xenobiotic Receptor)ノ アゴニスト カッセイ オ モツ シンキ ビタミン K ユウドウタイ ノ ゴウセイ ト コウゾウ カッセイ ソウカン ノ ケントウ

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Abstract

  Vitamin K2 is a ligand for a nuclear receptor, steroid and xenobiotic receptor (SXR), that induces the gene expressions of CYP3A4. We synthesized new vitamin K analogues with the same isoprene side chains symmetrically introduced at the 2 and 3 positions of 1,4-naphthoquinone and vitamin K2 analogues with hydroxyl or phenyl groups at the ω-terminal of the side chain. The upregulation of SXR-mediated transcription of the target gene by the analogues was dependent on the length of the side chain and the hydrophobicity of the ω-terminal residues. Phenyl analogue menaquinone-3 was as active as the known SXR ligand rifampicin.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 132 (8), 881-886, 2012-08-01

    The Pharmaceutical Society of Japan

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