Synthesis and structure-activity relationship study of diaryl[d, f][1,3]diazepines as potential anti-cancer agents

被引:13
|
作者
Yan, Longjia [1 ,2 ]
Wang, Hui [1 ,2 ]
Chen, Yunpeng [1 ,2 ]
Li, Zhiwei [1 ,2 ]
Pei, Yazhong [1 ,2 ]
机构
[1] Jilin Univ, Ctr Combinatorial Chem & Drug Discovery, Coll Chem, 1266 Fujin Rd, Changchun 130012, Jilin, Peoples R China
[2] Jilin Univ, Sch Pharmaceut Sci, 1266 Fujin Rd, Changchun 130012, Jilin, Peoples R China
基金
中国国家自然科学基金;
关键词
Benzo[1,3]diazepine; Diaryl[d, f][1,3]diazepine; Structure-activity relationship; Anti-cancer activity; KINASE INHIBITORS; DOPAMINE; ANTAGONIST; DISCOVERY; RECEPTORS; ECOPIPAM; DESIGN;
D O I
10.1007/s11030-017-9805-0
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We herein report the synthesis, biological activity and preliminary structure-activity relationships of a series of diaryl[1,3]diazepines. These compounds were able to inhibit the proliferation of many cancer cell lines, such as HeLa, MCF-7, SGC7901 and A549. When HeLa cells were treated with lead compounds 7j and 7k at 3 concentration, cell arrest was observed in the G2/M phase. [GRAPHICS] .
引用
收藏
页码:323 / 333
页数:11
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