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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.
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收藏
页码:17183 / 17190
页数:8
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