Synthesis and Antimetastatic Effects of E-Salignone Amide Derivatives

Authors

  • Hong-Ling Wang,

    1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China
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    • These authors contributed equally to this work.
  • Nan Qin,

    1. Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin, China
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    • These authors contributed equally to this work.
  • Jia Liu,

    1. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China
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  • Mei-Na Jin,

    1. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China
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  • Xiang Zhang,

    1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China
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  • Mei-Hua Jin,

    1. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China
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  • Dexin Kong,

    1. Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin, China
    2. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China
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  • Shen-De Jiang,

    1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China
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  • Hong-Quan Duan

    Corresponding author
    1. Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin, China
    2. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, China
    • Correspondence to: Hong-Quan Duan, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China.

      E-mail: duanhq@tijmu.edu.cn

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Abstract

Preclinical Research

The preparation of novel E-salignone derivatives and their biological evaluation as potential antimetastatic agents is described. The E-salignone amide derivatives were prepared from epiandrosterone and androsterone, and characterized by analytical 1H NMR, 13C NMR, and mass spectrometry. The derivatives were evaluated for antimetastatic activity in MDA-MB-231 cells by using a transwell assay. Comparing with the positive control, LY294002, compounds 19b, 19d, and 19e exhibited significant inhibitory effects on the EGF-induced invasion of MB-MDA-231 cells. Moreover, compound 19b also had antimigration effects in wound-healing assay. Compound 19b may represent a novel antimetastatic agent for treating breast cancer.

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