Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (12): 2933-2940.DOI: 10.6023/cjoc201604007 Previous Articles     Next Articles



崔建国a, 刘畅a, 刘亮b, 甘春芳a, 卢艳c, 陈爽a, 董新a, 黄燕敏a   

  1. a 北部湾环境演变与资源利用教育部重点实验室 广西师范学院化学与材料科学学院 南宁 530001;
    b 四川万之药业股份有限公司 成都 610041;
    c 广西防城港市高级中学 防城港 538001
  • 收稿日期:2016-04-04 修回日期:2016-06-17 发布日期:2016-08-12
  • 通讯作者: 甘春芳, 黄燕敏;
  • 基金资助:

    国家自然科学基金(Nos. 21562007,21462009)、广西高校科学研究(No. KY2015D077)及有机化学广西高校重点学科资助项目.

Synthesis and Antitumor Activities of Cholestane Derivatives with a Structure of 3-Hydroxy-6-hydrazone or 6-Carbonyl-3-hydrazone

Cui Jianguoa, Liu Changa, Liu Liangb, Gan Chunfanga, Lu Yanc, Chen Shuanga, Dong Xina, Huang Yanmina   

  1. a Key Laboratory of Beibu Gulf Environmental Change and Resources Utilization of Ministry of Education, College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001;
    b Sichuan Welltz Pharm Inc., Chengdu 610041;
    c Fangchenggan High School, Fangchenggang 538001
  • Received:2016-04-04 Revised:2016-06-17 Published:2016-08-12
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21562007, 21462009), the Science Research Project of Guangxi Teachers University (No. KY2015D077) and the Organic Chemistry in Guangxi University Key Disciplines.

Some cholestane hydrazone derivatives with a structure of 3-or 6-hydrazone group were synthesized by different chemical methods using cholesterol as a starting material, and their structures were characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds in vitro was evaluated against human Bel-7404 and SGC-7901 cancer cells. The results showed that the cholestane derivatives with the structure of 3-hydroxy-6-hydrazone exhibited distinct cytotoxicity. The information obtained from the studies is valuable for the design of novel steroidal chemotherapeutic drugs.

Key words: cholestane, hydrazone, heterocycle hydrazone, cholestane hydrazone, antiproliferative acitivity