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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

成伟华, 王文倩, 尚海, 张宏武, 郭强, 陈虹, 邹忠梅

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

  • 1.

    中国医学科学院北京协和医学院药用植物研究所

  • 2.

    原子高科股份有限公司

  • 3.

    天津药物研究院

  • 4.

    北京市计量检测科学研究院

  • 5.

    武警后勤学院生药学教研室

基金项目: 中国医学科学院医学与健康科技创新工程经费资助(No.2016-I2M-3-015),北京市自然科学基金资助项目(No.7142111)

Synthesis and cytotoxicity study of cembrane triazole derivatives

摘要

    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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    • 参考文献(14)
  • [1] Thao NP,Luyen BTT,Ngan NTT,et al.New anti-inflammatory cembranoid diterpenoids from the Vietnamese soft coral Lobophytum crassum[J].Bioorg Med Chem Lett,2014,24(1):228-232.
    [2] Peres MT,Delle Monache F,Cruz AB,et al.Chemical composition and antimicrobial activity of Croton urucurana Baillon(Euphorbiaceae)[J].J Ethnopharmacol,1997,56(3):223-226.
    [3] Tsacheva I,Rostan J,Iossifova T,et al.Complement inhibiting properties of dragon′s blood from Croton draco[J].Z Naturforsch C,2004,59(7/8):528-532.
    [4] Su JH,Ahmed AF,Sung PJ,et al.Manaarenolides AI,diterpenoids from the soft coral Sinularia manaarensis[J].J Nat Prod,2006,69(8):1134-1139.
    [5] Hassan HM,Sallam AA,Mohammed R,et al.Semisynthetic analogues of the marine cembranoid sarcophine as prostate and breast cancer migration inhibitors[J].Bioorg Med Chem,2011,19(16):4928-4934.
    [6] Fahmy H,Zjawiony JK,Konoshima T,et al.Potent skin cancer chemopreventing activity of some novel semi-synthetic cembranoids from marine sources[J].Mar Drugs,2006,4(2):28-36.
    [7] Huang HC,Ahmed AF,Su JH,et al.Crassocolides A-F,cembranoids with a transfused lactone from the soft coral Sarcophyton crassocaule[J].J Nat Prod,2006,69(11):1554-1559.
    [8] Sánchez MC,Ortega MJ,Zubía E,et al.Cembrane diterpenes from the gorgonian Lophogorgia peruana[J].J Nat Prod,2006,69(12):1749-1755.
    [9] Wen T,Ding Y,Deng Z,et al.Sinulaflexiolides A-K,cembrane-type diterpenoids from the Chinese soft coral Sinularia flexibilis[J].J Nat Prod,2008,71(7):1133-1140.
    [10] Cuzick J.Anastrozole[J].Drugs Today,2005: 41(4):227-239.
    [11] Ribatti D,Vacca A,Falco GD,et al.Angiogenesis and anti-angiogenesis in neuroblastoma[J].Eur J Cancer,2002,38(6):750-757.
    [12] Guo L,Li ZS,Wang HL,et al.Carboxyamido-triazole inhibits proliferation of human breast cancer cell via G2/M cell cycle arrest and apoptosis[J].Eur J Pharmacol,2006,538(1/2/3):15-22.
    [13] Cheng WH,Cao B,Shang H,et al.Synthesis and evaluation of novel podophyllotoxin derivatives as potential antitumor agents[J].Eur J Med Chem,2014,85:498-507.
    [14] Mahadevan D.Will MDR-1/P-gp modulators provide clinical benefit in hematologic malignancies[J]?Leuk Res,2006,30(9):1077-1078.
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  • 刊出日期:  2018-02-24

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