Squaramides with cytotoxic activity against human gastric carcinoma cells HGC-27: synthesis and mechanism of action

被引：17
|
作者：
Quintana, Mireia [1 ]
Alegre-Requena, Juan V. [1 ,2 ]
Marques-Lopez, Eugenia [2 ]
Herrera, Raquel P. [2 ]
Triola, Gemma [1 ]
机构：
[1] CSIC, Inst Adv Chem Catalonia IQAC, Biomed Chem Dept, E-08034 Barcelona, Spain
[2] Univ Zaragoza, CSIC, Lab Organocatalisis Asimetr, Dept Quim Organ,ISQCH, E-50009 Zaragoza, Spain
来源：
MEDCHEMCOMM | 2016年 / 7卷 / 03期
关键词：
ENANTIOSELECTIVE MICHAEL ADDITION; BIOLOGICAL EVALUATION; KINASE INHIBITORS; APOPTOSIS; DEATH; DERIVATIVES; DISCOVERY; AUTOPHAGY; TOXICITY; POTENT;
D O I：
10.1039/c5md00515a
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：
A series of squaramates and squaramides have been synthesized and their cytotoxic activity has been investigated in different cancer cell lines. Among the studied compounds, squaramide 34 showed a potent and selective cytotoxicity against the human gastric cancer cell line HGC-27. Studies directed to elucidate the mechanism of induced cell death were performed. Cell cycle distribution analysis and cell death studies showed that compound 34 induces cell cycle arrest at the G(1) phase and caspase-dependent apoptosis. In conclusion, squaramide 34 can be considered a potential anticancer agent for gastric carcinoma.
引用
收藏
页码：550 / 561
页数：12
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