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成伟华, 王文倩, 尚海, 张宏武, 郭强, 陈虹, 邹忠梅. 西松烷型二萜三氮唑衍生物的合成及其细胞毒活性[J]. 中国药科大学学报, 2018, 49(1): 56-63. DOI: 10.11665/j.issn.1000-5048.20180108
引用本文: 成伟华, 王文倩, 尚海, 张宏武, 郭强, 陈虹, 邹忠梅. 西松烷型二萜三氮唑衍生物的合成及其细胞毒活性[J]. 中国药科大学学报, 2018, 49(1): 56-63. DOI: 10.11665/j.issn.1000-5048.20180108
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CHENG Weihua, WANG Wenqian, SHANG Hai, ZHANG Hongwu, GUO Qiang, CHEN Hong, ZOU Zhongmei. Synthesis and cytotoxicity study of cembrane triazole derivatives[J]. Journal of China Pharmaceutical University, 2018, 49(1): 56-63. DOI: 10.11665/j.issn.1000-5048.20180108
Citation: CHENG Weihua, WANG Wenqian, SHANG Hai, ZHANG Hongwu, GUO Qiang, CHEN Hong, ZOU Zhongmei. Synthesis and cytotoxicity study of cembrane triazole derivatives[J]. Journal of China Pharmaceutical University, 2018, 49(1): 56-63. DOI: 10.11665/j.issn.1000-5048.20180108
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西松烷型二萜三氮唑衍生物的合成及其细胞毒活性

Synthesis and cytotoxicity study of cembrane triazole derivatives

    摘要
  • 摘要: 以从天然植物光叶巴豆叶醇提物中分离得到的具有一定抗肿瘤活性的西松烷型二萜化合物新巴豆瑞士松酸为先导化合物，设计并合成一系列含三氮唑的西松烷型二萜衍生物，合成12个新化合物，其结构经1H NMR、13C NMR和HRMS确定，采用MTT法考察所合成的目标化合物对HeLa，K562和K562/A02肿瘤细胞的抑制活性。活性测试结果表明，其中一些化合物具有细胞毒性。三氮唑引入西松烷型二萜后对耐药K562/A02细胞具有抗耐药活性。

     

    Abstract: A series of triazole derivatives were designed and synthesized based on a natural product cembrane separated from Croton laevigatus Vahl which showed potential antitumor activity against HeLa cells. Twelve novel compounds were synthesized and their structures were characterized by 1H NMR, 13C NMR and HRMS. Their cytotoxicities in vitro were evaluated for HeLa, K562 and K562/A02 cells by MTT assay. The results showed that some cembrane derivatives possessed antitumor activities. Substituted triazole connected to cembrane derivatives exhibited potent activity toward drug-resistant K562/A02 cells.

     

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