上海交通大学学报（医学版）

上海交通大学学报（医学版） ›› 2018, Vol. 38 ›› Issue (6): 605-.doi: 10.3969/j.issn.1674-8115.2018.06.004

• 论著·基础研究 • 上一篇    下一篇

以6,11-二氢-5H-苯并[a]咔唑优势结构为基础的抑制宫颈癌细胞增殖先导化合物的发现

董亚，杨若林，沈征武 ，刘坚华   

  1. 上海交通大学基础医学院化学教研室，上海 200025
  • 出版日期:2018-06-28 发布日期:2018-07-03
  • 通讯作者: 沈征武，电子信箱：jeff.shen@sjtu.edu.cn。刘坚华，电子信箱：jhliu7912@shsmu.edu.cn。为共同通信作者。
  • 作者简介:董亚（1993—），女，硕士生；电子信箱：DY1993@sjtu.edu.cn。
  • 基金资助:
    国家自然科学青年基金（81402775）；国家教育部博士点基金资助项目（20130073120113）

Discovery of lead compounds to inhibit proliferation of cervical cancer cells based on privileged structure of 6,11-dihydro-5H-benzo[a]carbazole

DONG Ya, YANG Ruo-lin, SHEN Zheng-wu, LIU Jian-hua   

  1. Department of Chemistry, Shanghai Jiao Tong University College of Basic Medical Sciences, Shanghai 200025, China
  • Online:2018-06-28 Published:2018-07-03
  • Supported by:
    National Natural Science Youth Fund, 81402775; PhD. Programs Foundation of Ministry of Education of China, 20130073120113

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摘要： 目的·发现以6,11-二氢-5H-苯并[a]咔唑环为母核可抑制宫颈癌细胞增殖的先导化合物。方法·用Fisher吲哚合成法制备了一系列6,11-二氢-5H-苯并[a]咔唑类化合物及其类似物，并在体外用CCK8法测试了这些化合物对HeLa细胞增殖的抑制作用。结果· 2-甲氧基-6,11-二氢-5H-苯并[a]咔唑和8-氯-2-甲氧基-6,11-二氢-5H-苯并[a]咔唑具有良好的抑制HeLa细胞增殖的活性，其半数抑制浓度（IC50）值分别为9.61 μmol/L和16.52 μmol/L。结论·发现2个目标先导化合物。在6,11-二氢-5H-苯并[a]咔唑类衍生物中，母环2位C上为甲氧基取代的衍生物具有较好的抗宫颈癌细胞增殖活性。

关键词: 6,11二氢-5H-苯并[a]咔唑类化合物, 优势结构, 宫颈癌, 先导化合物

Abstract:

Objective · To discover lead compounds with 6,11-dihydro-5H-benzo[a]carbazole as core scaffold that can inhibit the proliferation of cervical cancer cells. Methods · A series of 6,11-dihydro-5H-benzo[a]carbazole derivatives and analogs were synthesized using Fischer indole synthesis method, and their anticancer activity against HeLa cells was tested in vitroCCK8 test. Results · 2-Methoxy-6,11-dihydro-5H-benzo[a]carbazole and 8-chloro-2methoxy- 6,11-dihydro-5H-benzo[a]carbazole could significantly inhibit the proliferation of HeLa cells with the half maximal inhibitory concentration (IC50)values of 9.61 μmol/L and 16.52 μmol/L, respectively. Conclusion · Two objective lead compounds were found. Among 6,11-dihydro-5H-benzo[a]carbazole derivatives, compounds with methoxy group at the C-2 position of the core scaffold show better activity against proliferation of cervical cancer cells.

Key words: 6,11-dihydro-5H-benzo[a]carbazole analogues, privileged structure, cervical cancer, lead compound

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