Discovery of lead compounds to inhibit proliferation of cervical cancer cells based on privileged structure of 6,11-dihydro-5H-benzoacarbazole

VernacularTitle: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
Author: Ya DONG ¹ ; Ruo-Lin YANG ; Zheng-Wu SHEN ; Jian-Hua LIU
Author Information

1. 上海交通大学基础医学院化学教研室
Keywords: 6,11-dihydro-5H-benzo[a]carbazole analogues; privileged structure; cervical cancer; lead compound
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.