The antitumor activity of 4,4′-bipyridinium amphiphiles

被引：3
|
作者：
Wang, Senlin [1 ]
Wu, Hongshuai [1 ]
Chen, Fanghui [1 ]
Zhang, Yu [1 ]
Zhang, Yuchen [1 ]
Sun, Baiwang [1 ]
机构：
[1] Southeast Univ, Sch Chem & Chem Engn, Nanjing 211189, Jiangsu, Peoples R China
来源：
RSC ADVANCES | 2019年 / 9卷 / 57期
基金：
中国国家自然科学基金;
关键词：
CATIONIC ANTIMICROBIAL PEPTIDES; ANTICANCER PEPTIDES; CANCER; MECHANISMS;
D O I：
10.1039/c9ra06172j
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of 4,4 ' -bipyridinium amphiphiles were synthesized and their anticancer activities were further evaluated. MTT assay showed that the cytotoxicity first increased and then decreased with the growth of carbon chains (8-16 C) at both ends of bipyridyl. Specifically, compounds with saturated carbon chains consisting of 13 carbons at both ends of bipyridyl displayed the best cell inhibitory activity with IC50 values in the low-micromolar range, which were even superior to that of cisplatin, against all the tested human cancer cells and cisplatin-resistant A549 cancer cells in vitro. In addition, compound 6 could evidently arrest the G2/M phase of the cell cycle in a dose-dependent manner. Moreover, this study demonstrates the potent performance of compound 6 in cell growth inhibition and apoptosis induction via a conceivable approach of membrane damage.
引用
收藏
页码：33023 / 33028
页数：6
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