N-(4-哌啶基)苯甲酰胺衍生物的设计、合成及其抗肝癌活性

黄志宁 郑满意 苗方笑 于婧琦 李善花 李福男 曲宁

引用本文: 黄志宁, 郑满意, 苗方笑, 于婧琦, 李善花, 李福男, 曲宁. N-(4-哌啶基)苯甲酰胺衍生物的设计、合成及其抗肝癌活性[J]. 应用化学, 2016, 33(6): 661-667. doi: 10.11944/j.issn.1000-0518.2016.06.150358 shu
Citation:  HUANG Zhining, ZHENG Manyi, MIAO Fangxiao, YU Jingqi, LI Shanhua, LI Funan, QU Ning. Synthesis and Anti-hepatoma Activities of N-(Piperidin-4-yl)benzamide Derivatives[J]. Chinese Journal of Applied Chemistry, 2016, 33(6): 661-667. doi: 10.11944/j.issn.1000-0518.2016.06.150358 shu

N-(4-哌啶基)苯甲酰胺衍生物的设计、合成及其抗肝癌活性

    通讯作者: 曲宁,实验师;Tel:0592-2188672;Fax:0592-2181879;E-mail:quning@xmu.edu.cn;研究方向:分子生物学
  • 基金项目:

    福建省科技厅引导性(重点)(2015Y0081);厦门大学大学生创新创业训练计划(201510384055,20720152005)资助项目 

摘要: 以4-羟基苯甲酸乙酯为原料,经烃化、水解、缩合、脱保护、磺酰化反应,合成了6个含有磺酰基取代的4-苯氧基-N-(4-哌啶基)苯甲酰胺衍生物。其结构经1H NMR、13C NMR和MS谱等技术手段进行了表征,并以索拉非尼为阳性对照药对HepG2细胞株进行了初步体外抗肝癌细胞增殖活性的评价。实验发现,4-苯氧基-N-(1-甲磺酰基哌啶-4-基)苯甲酰胺的体外抗肝癌生物活性优于索拉非尼,IC50值为8.42 μmol/L。研究结果表明,新结构4-苯氧基-N-(4-哌啶基)苯甲酰胺类化合物具有良好的抗肝癌活性。

English

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  • 收稿日期:  2015-10-10
  • 网络出版日期:  2015-12-23
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