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2016 , Vol. 36 >Issue 6: 1431 - 1437

DOI: https://doi.org/10.6023/cjoc201512019

研究简报

新型含氟甲基吡唑结构的氰基丙烯酸酯类化合物的合成及其生物活性

  • 石玉军 ,
  • 李阳 ,
  • 方源 ,
  • 叶林玉 ,
  • 陈佳 ,
  • 戴红
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  • a 江苏科技大学环境与化学工程学院镇江 212003;
    b 南通大学化学化工学院南通 226019

收稿日期: 2015-12-14

  修回日期: 2016-01-07

  网络出版日期: 2016-02-02

基金资助

国家自然科学基金(Nos.21202089,21372135)、江苏省“六大人才高峰”(Nos.2011-SWYY-009,2013-SWYY-013)和南通市科技计划(Nos.AS2014011,CP12013002)资助项目.

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Synthesis and Bioactivity of Novel Cyanoacrylate Derivatives Containing Fluoride Methyl Pyrazole Moiety

  • Shi Yujun ,
  • Li Yang ,
  • Fang Yuan ,
  • Ye Linyu ,
  • Chen Jia ,
  • Dai Hong
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  • aSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang 212003;
    b College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019

Received date: 2015-12-14

  Revised date: 2016-01-07

  Online published: 2016-02-02

Supported by

Project supported by the National Natural Science Foundation of China (Nos. 21202089, 21372135), the Research Foundation of the Six People Peak of Jiangsu Province (Nos. 2011-SWYY-009, 2013-SWYY-013), and the Science and Technology Project Fund of Nantong City (Nos. AS2014011, CP12013002).

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摘要

为了从氰基丙烯酸酯类衍生物中寻找新的活性化合物, 采用活性亚结构拼接方法, 设计并合成了17个未见文献报道的新型含氟甲基吡唑结构的氰基丙烯酸酯类化合物. 利用1H NMR、13C NMR和元素分析对所制备的化合物的结构进行了表征. 此外, 利用MS证实了化合物7b、7f、7j和7o的结构. 初步的生物活性测试结果显示, 部分目标化合物表现出明显的抗肿瘤活性.

关键词： 含氟甲基吡唑; 氰基丙烯酸酯; 合成; 生物活性

本文引用格式

石玉军 , 李阳 , 方源 , 叶林玉 , 陈佳 , 戴红 . 新型含氟甲基吡唑结构的氰基丙烯酸酯类化合物的合成及其生物活性[J]. 有机化学, 2016 , 36(6) : 1431 -1437 . DOI: 10.6023/cjoc201512019

Abstract

In order to find novel cyanoacrylate lead compounds, 17 new cyanoacrylate compounds bearing fluoride methyl pyrazole moiety were synthesized by the method of active substructure combination. They were structurally confirmed by 1H NMR, 13C NMR and elemental analysis. The structures of compounds 7b, 7f, 7j and 7o were also tested through MS technique. Preliminary bioassay data showed that some of the target compounds displayed important anti-tumor activities.

Key words： fluoride methyl pyrazole; cyanoacrylate; synthesis; biological activity

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