Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (7): 1602-1610.DOI: 10.6023/cjoc201512031 Previous Articles     Next Articles

Articles

某些B-降胆甾噻唑化合物的合成及抗肿瘤活性研究

黄燕敏a, 戚斌斌a, 崔建国a,b, 甘春芳a, 杨春晖a, 刘畅a, 陈爽a, 石海信b   

  1. a. 广西师范学院化学与材料科学学院 南宁 530001;
    b. 广西高校北部湾石油天然气资源有效利用重点实验室 钦州学院 钦州 535000
  • 收稿日期:2015-12-23 修回日期:2016-03-05 发布日期:2016-03-25
  • 通讯作者: 崔建国, 石海信 E-mail:cuijg1954@126.com;shihaixin206@163.com
  • 基金资助:

    国家自然科学基金(No.2146209)和广西高校北部湾石油天然气资源有效利用重点实验室开放课题(No.2014KLOG09)资助项目.

Synthesis and Evaluation of Some New B-Norcholesteryl Thiazole Compounds as Anticancer Agents

Huang Yanmina, Qi Binbina, Cui Jianguoa,b, Gan Chunfanga, Yang Chunhuia, Liu Changa, Chen Shuanga, Shi Haixinb   

  1. a. College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001;
    b. Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resoure Effective Utilization, Qizhou University, Qizhou
  • Received:2015-12-23 Revised:2016-03-05 Published:2016-03-25
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21462009) and the Guangxi Colleges and University Key Laboratory Foundation of Beibu Gulf Oil and Natural Gas Resoure Effective Utilization (No. 2014KLOG09).

Some B-norcholesteryl thiazole compounds were synthesized and their structures were determined by IR, NMR and HRMS. The antiproliferative activity of the compounds against human lung carcinoma (A549), cervical carcinoma (HeLa), liver carcinoma (HEPG2) and normal kidney epithelial (HEK293T) cells was assayed. The results showed that some compounds with a structure of N-methylthiazole showed distinct antiproliferative activity against A549 and HEPG2 cells. The compounds with a structure of N-phenylthiazole displayed a selective antiproliferative activity against HeLa cells and were almost inactive to HEK293T cells. The research provided a theoretical reference for the exploration of new anti-cancer agents.

Key words: cholesterol, heterosteroids, B-norcholesteryl thiazoles, antiproliferative activity