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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (04): 611-616. 上一篇    下一篇

研究简报

3-芳基噻唑烷-4-酮-2-酰胺的合成及其抗肿瘤活性研究

陈华*，苑香果，秦占斌，赵建鹏，李小六*，张金超   

  1. (河北大学化学与环境科学学院 河北省化学生物学重点实验室 教育部药物化学与分子诊断省部共建重点实验室
    保定 071002)
  • 收稿日期:2009-08-06 修回日期:2009-11-13 发布日期:2010-04-28
  • 通讯作者: 陈华 E-mail:hua-todd@163.com
  • 基金资助:

    国家自然科学基金(20672027);河北省自然科学基金 (B2008000588);河北省科学技术研究与发展计划项目(09276418D-13);国家级.国家自然科学基金

Synthesis and Anti-tumor Study of 3-Aryl-4-oxo-thiazolidin- 2-carboxylic Acid Amides

Chen Hua* Yuan Xiangguo Qin Zhanbin Zhao Jianpeng Li Xiaoliu* Zhang Jinchao   

  1. (Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, College of Chemistry and Environmental Science, Hebei University, Baoding 071002)
  • Received:2009-08-06 Revised:2009-11-13 Published:2010-04-28

PDF

1253

被引次数

19 | 5

合成了系列新的3-芳基噻唑烷-4-酮-2-酰胺衍生物, 并测试了化合物抑制肿瘤细胞增殖活性. 部分化合物对A-549和Hela肿瘤细胞有弱的细胞毒性, 而对BGC-823没有抑制作用, 表现出一定的选择性. 其中, 化合物7ad对A-549有较强的抑制活性(IC50＝21.0 μmol•L－1), 与阳性对照顺铂的抑制活性(IC50＝19.4 μmol•L－1)相当. 初步的构效关系表明化合物的立体结构可能对其抗肿瘤活性影响较大.

关键词: 噻唑烷-4-酮, 合成, 细胞毒性, 肿瘤细胞, 构效关系

A series of novel 3-aryl-4-oxo-thiazolidin-2-carboxylic acid amides were synthesized and evaluated for their antiproliferative activity for three tumor cells. Some compounds showed weak cytotoxicity against A-549 and Hela tumor cells, but no antiproliferative activity against BGC-823, which suggested such compounds with a certain cytotoxicity selectivity to the three tumor cells. Among them, compound 7ad was the best one against A-549 with the IC50 value of 21.0 μmol•L－1, nearly equivalent to that of the positive control cisplatin (IC50＝19.4 μmol•L－1). Preliminary structure activity relationship analysis of these analogues suggested that the steric factor may be important to the anti-tumor activity.

Key words: thiazolidin-4-one, synthesis, cytotoxic activity, tumor cell, structure-activity relationship