| β-西柏三烯衍生物的合成及抗肿瘤活性 |
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| 引用本文： | 杨静,白冰,王龙,张改红,毛多斌.β-西柏三烯衍生物的合成及抗肿瘤活性[J].化学研究与应用,2022,34(1):78-84. |
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| 作者姓名： | 杨静 白冰 王龙 张改红 毛多斌 |
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| 作者单位： | 郑州轻工业大学食品与生物工程学院,河南 郑州 450000;湖北中烟工业有限责任公司,湖北 武汉 430000 |
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| 基金项目： | 国家烟草专卖局行业重点实验室基金项目(中烟办[2014]334号)资助。 |
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| 摘 要： | 为了提高大环二萜类化合物β-2,7,11-西柏三烯-4,6-二醇(β-CBT)的活性,对其C-6位羟基进行酯化、醚化修饰,合成了11个未见活性报道的化合物,利用1H NMR,13CNMR,IR,HR-MS对目标化合物结构进了表征。对合成的化合物进行了体外抗肿瘤活性评价,结果显示,部分化合物对白血病HL-60和肺癌A-549肿瘤细胞的具有一定的抑制作用,其中β-2,7,11-西柏三烯-4-醇-6-O-苯甲酸酯(1g)对HL-60以及β-2,7,11-西柏三烯-4-醇-6-O-乙基(2b)对肺癌细胞株SMMC-7721 IC50值分别为12.59和26.56μmol·L-1,显著高于母体化合物。
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| 关 键 词： | β-西柏三烯 衍生物 抗肿瘤 |
Synthesis and anticancer activities of β-2 ,7 , 11-cembratriene-4 ,6-diol derivatives |
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| YANG Jing,BAI Bing,WANG Long,Zhang Gai-hong,MAO Duo-bin.Synthesis and anticancer activities of β-2 ,7 , 11-cembratriene-4 ,6-diol derivatives[J].Chemical Research and Application,2022,34(1):78-84. |
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| Authors: | YANG Jing BAI Bing WANG Long Zhang Gai-hong MAO Duo-bin |
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| Institution: | (School of Food&Biological Engineering,Zhengzhou University of Light Industry,Zhengzhou 450000,China;China Tobacco Hubei Industrial Co.,Ltd.,Wuhan 430000,China) |
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| Abstract: | In order to find high-efficiency anti-tumor drugs,β-2,7,11-cembratriene-4,6-diol derivatives were prepared by a modification at C-6 position via introduction with acyl and ether groups.Their structures were confirmed by 1H NMR,13C NMR,IR and HR-MS.The synthesized compounds were screened for their in vitro anticancer activity with MTS assay.The results indicated that some of them showed moderate activity.The anticancer activities ofβ-2,7,11-cembratriene-4-ol-6-benzoate(1g)against HL-60 with IC50 value of 12.59μmol·L-1,andβ-2,7,11-cembratriene-4-ol-6-ethyl(2b)against A-549 with IC50 value of 26.56μmol·L-1,which was better than the parent compound. |
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| Keywords: | β-cembratriene derivatives cytotoxicity |
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