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新型1,1-二氧代-4H-苯并[1,2,4]-噻二嗪类衍生物的合成及其抗肿瘤活性

谭绪霞 ,  李世宁 ,  赵杰 ,  毛伸 ,  毛龙飞 ,  徐桂清

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引用本文: 谭绪霞, 李世宁, 赵杰, 毛伸, 毛龙飞, 徐桂清. 新型1,1-二氧代-4H-苯并[1,2,4]-噻二嗪类衍生物的合成及其抗肿瘤活性[J]. 应用化学, 2016, 33(9): 1067-1072. doi: 10.11944/j.issn.1000-0518.2016.09.150420 shu
Citation:  TAN Xuxia, LI Shining, ZHAO Jie, MAO Shen, MAO Longfei, XU Guiqing. Synthesis and Antitumor Activity of Novel 4H-1,2,4-Benzothiadiazine 1,1-Dioxide Derivatives[J]. Chinese Journal of Applied Chemistry, 2016, 33(9): 1067-1072. doi: 10.11944/j.issn.1000-0518.2016.09.150420 shu

新型1,1-二氧代-4H-苯并[1,2,4]-噻二嗪类衍生物的合成及其抗肿瘤活性

  • 1.

    a 河南师范大学化学化工学院 河南 新乡 453007;

  • 2.

    b 天方药业有限公司 河南 驻马店 463000

    • 通讯作者: 徐桂清,副教授;Tel:0373-3329121;E-mail:guiqingxu@163.com;研究方向:药物化学
  • 基金项目:

    国家自然科学基金（21402043）；河南省产学研项目（132107000035） 

摘要: 以2-硝基苯磺酰氯为起始原料，经多步反应合成了12种新型1，1-二氧代-4H-苯并[1，2，4]-噻二嗪类衍生物，产物收率高，水溶性好，并经1H NMR、13C NMR、MS-ESI和元素分析法确证结构。用MTT法测试了这类衍生物对肝癌细胞HepG-2生长的抑制作用，结果显示目标化合物能不同程度地抑制肿瘤细胞生长，其中7-氨甲基-3-环丙基-1，1-二氧代-4H-苯并[1，2，4]-噻二嗪（7c）对肝癌细胞HepG-2的抗性显著，最高抑制率达到79.3%。

English

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  • 收稿日期:  2015-11-30
  • 网络出版日期:  2016-03-24
通讯作者: 陈斌, bchen63@163.com
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