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

页码：17183 / 17190

页数：8

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