Discovery of lead compounds to inhibit proliferation of cervical cancer cells based on privileged structure of 6,11-dihydro-5H-benzoacarbazole
10.3969/j.issn.1674-8115.2018.06.004
- Author:
Ya DONG
1
Author Information
1. Department of Chemistry, Shanghai Jiao Tong University College of Basic Medical Sciences
- Publication Type:Journal Article
- Keywords:
6,11-dihydro-5H-benzo[a]carbazole analogues;
Cervical cancer;
Lead compound;
Privileged structure
- From:
Journal of Shanghai Jiaotong University(Medical Science)
2018;38(6):605-609
- CountryChina
- Language:Chinese
-
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 vitro by CCK8 test. Results • 2-Methoxy-6,11-dihydro-5H-benzo[a]carbazole and 8-chloro-2- methoxy-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.
