Journal of Shanghai Jiao Tong University (Medical Science) >

2018 , Vol. 38 >Issue 6: 605

DOI: https://doi.org/10.3969/j.issn.1674-8115.2018.06.004

Original article (Basic research)

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
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  • Department of Chemistry, Shanghai Jiao Tong University College of Basic Medical Sciences, Shanghai 200025, China

Online 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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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

Cite this article

DONG Ya , YANG Ruo-lin , SHEN Zheng-wu , LIU Jian-hua . Discovery of lead compounds to inhibit proliferation of cervical cancer cells based on privileged structure of 6,11-dihydro-5H-benzo[a]carbazole[J]. Journal of Shanghai Jiao Tong University (Medical Science), 2018 , 38(6) : 605 . DOI: 10.3969/j.issn.1674-8115.2018.06.004

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