Synthesis of New Vitamin K Analogues as Steroid and Xenobiotic Receptor (SXR) Agonists: Insights into the Biological Role of the Side Chain Part of Vitamin K

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• 作者：Yoshitomo Suhara ; Masato Watanabe ; Sayaka Motoyoshi ; Kimie Nakagawa ; Akimori Wada ; Kazuyoshi Takeda ; Kazuhiko Takahashi ; Hiroaki Tokiwa ; Toshio Okano
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：July 14, 2011
• 年：2011
• 卷：54
• 期：13
• 页码：4918-4922
• 全文大小：766K
• 年卷期：v.54,no.13(July 14, 2011)
• ISSN：1520-4804

文摘

Vitamin K₂ has been demonstrated to induce gene expression related to bone formation through a nuclear steroid and xenobiotic receptor (SXR). 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 evaluated the transcriptional activity of the target gene. The transcriptional activity was related to the length of the side chain which allowed optimal interaction with ligand-binding domain of SXR.