Synthesis of 24,24-Difluoro-1,3-cis-25-dihydroxy-19-norvitamin D₃ Derivatives and Evaluation of Their Vitamin D Receptor-Binding Affinity

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  • Biswas Tanima
    Faculty of Advanced Science and Engineering, Waseda University
  • Akagi Yusuke
    Graduate School of Technology, Tokyo University of Agriculture and Technology
  • Usuda Kosuke
    Graduate School of Technology, Tokyo University of Agriculture and Technology
  • Yasui Koji
    Graduate School of Technology, Tokyo University of Agriculture and Technology
  • Shimizu Isao
    Faculty of Advanced Science and Engineering, Waseda University
  • Okamoto Mayumi
    Faculty of Advanced Science and Engineering, Waseda University Department of Immunology and Pathology, Research Institute, National Center for Global Health and Medicine
  • Uesugi Motonari
    Institute for Integrated Cell-Material Sciences (WPI-iCeMS), Kyoto University Institute for Chemical Research, Kyoto University
  • Hosokawa Seijiro
    Faculty of Advanced Science and Engineering, Waseda University
  • Nagasawa Kazuo
    Graduate School of Technology, Tokyo University of Agriculture and Technology

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  • Synthesis of 24,24-Difluoro-1,3-<i>cis</i>-25-dihydroxy-19-norvitamin D<sub>3</sub> Derivatives and Evaluation of Their Vitamin D Receptor-Binding Affinity

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<p>Two vitamin D3 derivatives, namely 24,24-difluoro-1β,3β,25-dihydroxy-19-norvitamin D3 (6a) and 24,24-difluoro-1α,3α,25-dihydroxy-19-norvitamin D3 (6b), were synthesized via a convergent route employing Julia–Kocienski olefination as a key step. Compounds 6a and b bound to vitamin D receptor (VDR) with IC50 values of 64.8 and 57.6 nM, respectively, exhibiting about 400- and 30-fold greater binding affinity than the corresponding non-fluorinated derivatives 5a and b.</p>

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