Synthesis and antitumor activity of novel 2-substituted indoline imidazolium salt derivatives

被引:35
|
作者
Xu, Xiao-Liang [1 ]
Yu, Chun-Lei [2 ]
Chen, Wen [1 ]
Li, Ying-Chao [1 ]
Yang, Li-Juan [3 ,4 ]
Li, Yan [2 ]
Zhang, Hong-Bin [1 ]
Yang, Xiao-Dong [1 ]
机构
[1] Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China
[2] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Peoples R China
[3] Yunnan Minzu Univ, State Ethn Affairs Commiss, Key Lab Ethn Med Resource Chem, Kunming 650500, Peoples R China
[4] Yunnan Minzu Univ, Minist Educ, Kunming 650500, Peoples R China
关键词
CYTOTOXIC ACTIVITIES; HYBRID COMPOUNDS; DESIGN; CHECKPOINT; AGENTS; TRANS;
D O I
10.1039/c4ob02385d
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of novel 2-substituted indoline imidazolium salt derivatives has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of a substituted benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or 2-naphthylmethyl group were vital for modulating the cytotoxic activity. Compound 25 was found to be the most potent derivative with IC50 values of 0.24-1.18 mu M, and exhibited cytotoxic activity selectively against MCF-7, SW480, SMMC-7721 and HL-60 cell lines, while compound 26 showed powerful inhibitory activities selectively against SMMC-7721 and A549 cell lines. Compound 25 can induce G2/M phase cell cycle arrest and apoptosis in SMMC-7721 cells.
引用
收藏
页码:1550 / 1557
页数:8
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