Synthesis and Biological Evaluation of Pyridooxazine-Tetrahydroisoquinoline Derivatives as MDR Modulators

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著者

    • MA Chen
    • School of Chemistry and Chemical Engineering, Shandong University
    • LIU Shao-Jie
    • School of Chemistry and Chemical Engineering, Shandong University
    • XIN Liang
    • School of Chemistry and Chemical Engineering, Shandong University
    • ZHANG Qun
    • School of Chemistry and Chemical Engineering, Shandong University
    • DING Kai
    • School of Chemistry and Chemical Engineering, Shandong University
    • FALCK J. R.
    • Department of Biochemistry, University of Texas Southwestern Medical Center

抄録

Pyridooxazine–tetrahydroisoquinoline derivatives were designed and synthesized for MDR modulating activity. Pyridooxazin-2-one scaffolds were constructed in a one-pot annulation of <I>N</I>-substituted-2-chloroacetamides with 2-bromo-3-hydroxy pyridine via Smiles rearrangement. The Pictet–Spengler cyclization to form tetrahydroisoquinoline ring afforded target compounds in 17–37% overall yields. Some of these compounds exhibited multidrug resistance (MDR) reversing activity.

収録刊行物

  • Chemistry letters  

    Chemistry letters 35(9), 1010-1011, 2006-09-05 

    The Chemical Society of Japan

参考文献:  24件

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各種コード

  • NII論文ID(NAID)
    10018062952
  • NII書誌ID(NCID)
    AA00603318
  • 本文言語コード
    ENG
  • 資料種別
    SHO
  • ISSN
    03667022
  • データ提供元
    CJP書誌  J-STAGE 
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