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首页> 外文期刊>RSC Advances >Synthesis of novel natural product-like diaryl acetylenes as hypoxia inducible factor-1 inhibitors and antiproliferative agents
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Synthesis of novel natural product-like diaryl acetylenes as hypoxia inducible factor-1 inhibitors and antiproliferative agents

机译：作为缺氧诱导因子-1抑制剂和抗增殖剂的新型天然产物样用金属酰乙炔合成

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摘要

The selaginellin derivatives are a type of novel natural pigments with an unusual alkynyl phenol skeleton from the genus Selaginella. Some of these natural compounds were previously reported to show important bioactivities, including anticancer activity, cardiovascular protection and phosphodiesterase-4 inhibition. We designed and synthesized fifteen biphenyl-containing diaryl acetylene derivatives mimicking the skeleton of natural alkynyl phenols. In MTT assay in cancer cells, compounds 1c, 2d, 2g, 2h, 2i and 2j exhibited potent antiproliferative activity. The evaluation of Hypoxia Inducible Factor-1 (HIF-1) pathway inhibitory activity in dual luciferase assay demonstrated that most tested compounds exhibited moderate to good activities. Compounds 1a, 2f and 2h displayed high HIF-1 inhibitory activities and relatively low cytotoxicity, demonstrating great potential as HIF-1 inhibitors. These results afford a new strategy for the discovery of new HIF-1 inhibitors and anti-proliferative agents from natural or synthetic diaryl acetylene derivatives.
机译：SelAginellin衍生物是一种新型天然颜料，具有来自Selaginella属的异常炔基苯酚骨架。先前，这些天然化合物中的一些是为了显示重要的生物活化，包括抗癌活性，心血管保护和磷酸二酯酶-4抑制。我们设计和合成了含15个含二苯基的含二烯基的二芳基乙炔衍生物，其模仿天然炔基酚的骨架。在癌细胞中的MTT测定中，化合物1c，2d，2g，2h，2i和2j表现出有效的抗增殖活性。双荧光素酶测定中缺氧诱导因子-1（HIF-1）途径抑制活性的评价表明，大多数测试的化合物表现出中等至良好的活性。化合物1A，2F和2H显示出高HIF-1抑制活性和相对低的细胞毒性，展示了HIF-1抑制剂的巨大潜力。这些结果提供了一种从天然或合成二芳基乙炔衍生物发现新的HIF-1抑制剂和抗增殖药的新策略。

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  • 来源
    《RSC Advances》 |2019年第24期|共9页
  • 作者

    Wang Shisheng; Liu Liqiang; Guo Xiuhan; Li Guangzhe; Wang Xu; Dong Huijuan; Li Yueqing; Zhao Weijie;

  • 作者单位

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

    Dalian Univ Technol Sch Chem Engn Dept Pharm Dalian 116023 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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