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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (11): 1432-1437. 上一篇    下一篇

研究简报

噁唑、苯并噁唑及1,3,4-噁二唑硫醚的合成及抗肿瘤活性研究

张成仁，王柳，葛燕丽，巨修练*   

  1. (武汉工程大学化工与制药学院 湖北省新型反应器与绿色化学工艺重点实验室 武汉 430073)
  • 收稿日期:2006-10-08 修回日期:2007-03-20 发布日期:2007-10-20
  • 通讯作者: 巨修练

Synthesis and Antitumor Activity of Oxazol-2-yl, Benzoxazol-2-yl and 1,3,4-Oxadiazol-2-yl Sulfur Ethers

ZHANG Cheng-Ren,WANG Liu,GEYan-Li,JU Xiu-Lian*   

  1. (Hubei Key Laboratory of Novel Chemical Reactor and Green Chemical Technology, School of Chemical Engi-neering and
    Pharmacy, Wuhan Institute of Technology, Wuhan 430073)
  • Received:2006-10-08 Revised:2007-03-20 Published:2007-10-20
  • Contact: JU Xiu-Lian

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被引次数

81 | 20

设计并以噁唑、苯并噁唑及1,3,4-噁二唑硫醇与卤代烃反应合成了14个硫醚类杂环化合物, 其中13个化合物未见文献报道. 目标化合物的结构均通过1H NMR谱、MS和元素分析进行了表征. 采用MTT [3-(4,5-dimethylthiagol-2-yl)- 2,5-diphenyltetrogolium bromide]法对14个目标化合物进行了体外抗肿瘤活性测定, 结果表明: 在10－5 mol/L 浓度下, 10个化合物对肿瘤细胞具有抑制活性.

关键词: 噁唑, 苯并噁唑, 1,3,4-噁二唑, 抗肿瘤活性, 硫醚

14 heterocylic sulfur ethers were designed and synthesized by the reaction of 2-thiol-oxazoles, 2-thiol-benzoxazoles and 2-thiol-1,3,4-oxadiazoles with alkyl halides, respectively, and those of 13 com-pounds have not been reported. All compounds were characterized by MS, 1H NMR spectra and elemental analysis. The preliminary antitumor activities were investigated by MTT method and the results show that 10 compounds display a content of antitumor activity at the concentration of 10－5 mol/L.

Key words: benzoxazole, 1,3,4-oxadiazole, antitumor activity, sulfur ether, oxazole