›› 2018, Vol. 38 ›› Issue (6): 605-.doi: 10.3969/j.issn.1674-8115.2018.06.004

• Original article (Basic research) • Previous Articles     Next Articles

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

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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