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3-取代-12-氧代-N, N-双(2-氯乙基)脱氧胆酰胺的合成及其抑制癌细胞活性

甘春芳1,苏绍烊2,黄燕敏1,林啟福1,崔建国1*   

  1. (1.广西师范学院化学与生命科学学院 南宁 530001；2.广西特种设备监督检验院 南宁 530219)
  • 收稿日期:2012-08-16 修回日期:2012-11-08 出版日期:2013-06-10 发布日期:2013-06-10
  • 通讯作者: 崔建国，教授; Tel:0771-3908065; E-mail:cuijg1954@126.com; 研究方向：有机化学
  • 作者简介:
  • 基金资助:
    广西自然科学基金(2010GXNSFD013019)和广西教育厅自然科学基金(201202ZD059)资助项目

Synthesis and Antiproliferative Activity of 3-Substituted-12-oxy-N,N-bis-(2-chloroethyl)-7-deoxycholic Amides

GAN Chunfang1, SU Shaoyang2, HUANG Yanmin1, LIN Qifu1, CUI Jianguo1*   

  1. (1.College of Chemistry and Life Science,Guangxi Teachers Education University,Nanning 530001,China;
    2.Guangxi Special Equipment Supervision and Inspection Institute,Nanning 530219,China)
  • Received:2012-08-16 Revised:2012-11-08 Published:2013-06-10 Online:2013-06-10

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被引次数

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摘要： 以7-脱氧胆酸(1)为原料,由Jones试剂氧化得到3,12-二氧代-7-脱氧胆酸(2)，然后与双(2-氯乙基)胺反应，得到3,12-二氧代-N,N-双(2-氯乙基)-7-脱氧胆酰胺(4)，进一步通过对化合物4中的3-位羰基进行官能团转换，得到2个3-位分别被肟基、缩胺硫腙基取代的12-氧代-N,N-双(2-氯乙基)-7-脱氧胆酰胺类型化合物。 同时，初步测试了合成物对肿瘤细胞增殖抑制活性，结果表明，化合物对宫颈癌细胞的生长有显著的抑制活性。

关键词: 脱氧胆酸, 氮芥, 合成, 抗肿瘤活性

Abstract: Using 7-deoxycholic acid(1) as a starting material, 3,12-dioxy-7-deoxycholic acid(2) was obtained by oxidation with Jones reagent. Then the N,N-bis(2-chloroethyl)-3,12-dioxy-7-deoxycholic amide(4) was synthesized by the reaction of compound 2 with bis(2-chloroethyl)amine. Furthermore, N,N-bis(2-chloroethyl)-12-oxy-3-hydroximino-7-deoxycholic amide(5) and N,N-bis(2-chloroethyl)-12-oxy-3-thiosemicarbazone-7-deoxycholic amide(6) were prepared by the functional group transformation of 3-carbonyl on compound 4. The antiproliferative activities of compounds against HeLa cells were assayed and the result showed that the compounds displayed distinct cytotoxicity.

Key words: deoxycholic acid, substituted-oxy-N,N-bis(chloroethyl)-deoxycholic amides, synthesis, antitumor activity

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