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Synthesis and biological evaluation of amino acid derivatives containing chrysin that induce apoptosis

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成果类型:
期刊论文
作者:
Li, Yang;Zhang, Qizhi;He, Jun;Yu, Wenmei;Xiao, Jie;...
通讯作者:
Liu, Yunmei
作者机构:
[Li, Yang; Zhang, Qizhi; Yu, Wenmei; Xiao, Jie; Guo, Yu; Liu, Yunmei] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China
[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang, Peoples R China
[Zhu, Xiaoming] Hengyang Normal Univ, Inst Chem & Mat Sci, Hengyang, Peoples R China
通讯机构:
[Liu, Yunmei] U
Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
语种:
英文
关键词:
Chrysin derivatives;amino acid;apoptosis;breast cancer;cell viability
期刊:
Natural Product Research
ISSN:
1478-6419
年:
2019
卷:
35
期:
4
页码:
529-538
基金类别:
Hunan Natural Science Foundation Project [2018JJ2349]; University of South China Students Research Learning and Innovative Experimental Project [2018147200]; Graduate student science foundation of University of South China [2018496]
机构署名:
本校为第一且通讯机构
院系归属:
化学化工学院
药学与生物科学学院
摘要:
A series of chrysin amino acid derivatives were synthesized to evaluate for their antiproliferative activities against several cancer cell lines. Among the compounds tested, N-(2-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)octanoyl)-L-leucine methyl ester(5d) presented a good anti-proliferative activity in MDA-MB-231 and MCF-7 cells. Flow cytometry analysis showed that 5d induced apoptosis and prolonged cell cycle progression in MDA-MB-231 and MCF-7 cells. Western blot analysis showed that 5d significantly inhibited Akt phosphorylation (Ser473) in MDA-MB-231 and MCF-7 cells. In addition, 5d...

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