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2012 >Issue 03: 593 - 596

DOI: https://doi.org/10.6023/cjoc1101201

研究简报

烷基杂环芳基二硫醚类化合物的合成及抗癌活性研究

  • 龚景旭 ,
  • 盛丽 ,
  • 姚励功 ,
  • 李佳 ,
  • 周宇波 ,
  • 郭跃伟
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  • 中国科学院上海药物研究所 新药研究国家重点实验室 上海 201203

收稿日期: 2011-01-20

  修回日期: 2011-11-08

  网络出版日期: 2012-03-24

基金资助

国家新药创制重大专项(No. 2009ZX09301-00, 2009ZX09103-060)、国家自然科学基金(Nos. 81072572, 21072204, 21021063)、国家海洋“863”计划(No.2011AA09070102)、上海市科委基础研究(Nos. 09ZR1438000, 10540702900)和中国科学院重点(Nos. KSCX2-EW-R-15, KSCX2-YW-R-18)资助项目.

收起

Synthesis and Anti-tumor Activity Evaluation of Alkyl Heterocyclyl Disulfides

  • Gong Jingxu ,
  • Sheng Li ,
  • Yao Ligong ,
  • Li Jia ,
  • Zhou Yubo ,
  • Guo Yuewei
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  • State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203

Received date: 2011-01-20

  Revised date: 2011-11-08

  Online published: 2012-03-24

Supported by

Project supported by the National S & T Major Project (Nos. 2009ZX09301-001, 2009ZX09103-060), the Natural Science Foundation of China (Nos. 81072572, 21072204, 21021063), the National Marine “863” Project (No. 2011AA09070102), the Basic Research Project of Shanghai Science and Technology Commission (Nos. 09ZR1438000, 10540702900), and the Key Program of the Chinese Academy of Sciences (Nos. KSCX2-EW-R-15, KSCX2-YW-R-18).

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摘要

通过Bunte 盐与杂环芳基硫醇反应, 得到了一系列的烷基芳基二硫醚类化合物. 得到的全部二硫醚类化合物对人结肠癌细胞HCT-116 抑制活性进行了体外评价, 发现所有化合物具有明显的体外抗肿瘤活性, 其半抑制浓度IC50 为4.8～17.7 μg·mL-1.

关键词： 二硫醚; 合成; 抗肿瘤活性

本文引用格式

龚景旭 , 盛丽 , 姚励功 , 李佳 , 周宇波 , 郭跃伟 . 烷基杂环芳基二硫醚类化合物的合成及抗癌活性研究[J]. 有机化学, 2012 , (03) : 593 -596 . DOI: 10.6023/cjoc1101201

Abstract

A series of alkyl heterocyclyl disulfides were prepared by reaction of the heterocyclyl thiol with Bunte salts. All the synthesized compounds showed interesting inhibit activities toward human colon carcinoma cells (HCT-116) in vitro. The IC50 values of the tested compounds ranged from 4.8 μg·mL-1 to 17.7 μg·mL-1.

Key words： disulfides; synthesis; anti-tumor activity

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