Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents

被引:16
|
作者
You, Xin [1 ]
Zhu, Daqian [1 ,2 ]
Lu, Wenhua [1 ]
Sun, Yichen [1 ]
Qiao, Shuang [1 ,2 ]
Luo, Bingling [1 ,2 ]
Du, Yongliang [1 ,2 ]
Pi, Rongbiao [2 ]
Hu, Yumin [1 ]
Huang, Peng [1 ]
Wen, Shijun [1 ,2 ]
机构
[1] Sun Yat sen Univ, Canc Ctr, Collaborat Innovat Ctr Canc Med, State Key Lab Oncol South China, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China
[2] Sun Yat Sen Univ, Sch Pharmaceut Sci, 132 Waihuan East Rd, Guangzhou 510006, Guangdong, Peoples R China
来源
RSC ADVANCES | 2018年 / 8卷 / 31期
基金
中国国家自然科学基金;
关键词
CYCLIC DIARYLIODONIUM SALTS; DNA-DAMAGE CHECKPOINTS; CELL-CYCLE; OXIDATIVE STRESS; CANCER-CELLS; APOPTOSIS; INHIBITION; ALKALOIDS; DISCOVERY; ALKYNES;
D O I
10.1039/c8ra02939c
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In this work, a set of structurally diverse synthetic carbazoles was screened for their anticancer activities. According to structure-activity relationship studies, carbazoles with an N-substituted sulfonyl group exhibited better anticancer activity. Moreover, compound 8h was discovered to show the most potent anticancer effects on Capan-2 cells by inducing apoptosis and cell cycle arrest in G2/M phase. Finally, the in vivo study demonstrated that 8h prevented the tumor growth in PANC-1 and Capan-2 xenograft models without apparent toxicity.
引用
收藏
页码:17183 / 17190
页数:8
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