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2012 , Vol. 70 >Issue 02: 151 - 160

DOI: https://doi.org/10.6023/A1105302

研究论文

新型含噁二唑环的苯并噁/噻唑啉酮衍生物的合成、表征及生物活性

  • 李英俊 ,
  • 李春燕 ,
  • 靳焜 ,
  • 孙淑琴 ,
  • 周晓霞
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  • a 辽宁师范大学化学化工学院 大连 116029;
    b 大连理工大学精细化工国家重点实验室 大连 116012

收稿日期: 2011-05-30

  修回日期: 2011-07-25

  网络出版日期: 2012-02-25

基金资助

辽宁省自然科学基金(No.20102126)资助项目.

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Synthesis and Biological Activities of Novel Benzoxazolinone/Benzothiazolone Derivatives Containing Oxadiazole Moiety

  • LI Ying-Jun ,
  • LI Chun-Yan ,
  • JIN Kun ,
  • SUN Shu-Qin ,
  • ZHOU Xiao-Xia
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  • a College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029;
    b State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012

Received date: 2011-05-30

  Revised date: 2011-07-25

  Online published: 2012-02-25

Supported by

Project supported by the Natural Science Foundation of Liaoning Province (No.20102126).

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摘要

以邻氨基苯酚(硫酚)和尿素为起始原料, 经一系列反应, 合成出了30个新型含噁二唑环的苯并噁/噻唑啉酮衍生物(6). 利用IR、1H NMR 和元素分析对新化合物4 和6 的结构进行了表征. 对所合成的目标化合物进行了抗癌、抗炎和免疫调节活性的筛选, 实验结果表明, 部分目标化合物具有弱的抗癌和免疫调节活性, 对TNF-α 和Cdc25B 磷酸酯酶均无抑制活性.

关键词： 苯并噁/噻唑啉酮; 噁二唑; 合成; 表征; 生物活性

本文引用格式

李英俊 , 李春燕 , 靳焜 , 孙淑琴 , 周晓霞 . 新型含噁二唑环的苯并噁/噻唑啉酮衍生物的合成、表征及生物活性[J]. 化学学报, 2012 , 70(02) : 151 -160 . DOI: 10.6023/A1105302

Abstract

Thirty novel benzoxazolinone/benzothiazolone derivatives (6) containing oxadiazole moiety were synthesized by 2-aminophenol or 2-minothiophenol and urea as starting materials via a series of reactions. The structures of new intermediate 4 and the target compounds 6 were characterized by IR, 1H NMR spectra and elemental analysis. The synthesized target compounds were screened for the anticancer, antiinflammatory and immunoregulatory activities. The results indicated that some compounds exhibited weak activities in the anticancer and immunoregulatory fields, while all of them were found to be inactive against TNF-α and Cdc25B phosphatase.

Key words： benzoxazolinone/benzothiazolone; oxadiazole; synthesis; characterization; bioactivity

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