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Design, synthesis, and preliminary biological evaluation of chrysin amino acid derivatives that induce apoptosis and suppress cell migration

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成果类型:
期刊论文
作者:
Liu, Yun-Mei*;Li, Yang;Xiao, Jie;Zhang, Qi-Zhi;Song, Jian-Xin*
通讯作者:
Liu, Yun-Mei;Song, Jian-Xin
作者机构:
[Liu, Yun-Mei; Song, Jian-Xin] Hunan Normal Univ, Key Lab Assembly & Applicat Organ Funct Mol Hunan, Minist Educ China, Key Lab Chem Biol & Tradit Chinese Med, Changsha 410081, Hunan, Peoples R China.
[Xiao, Jie; Liu, Yun-Mei; Li, Yang; Zhang, Qi-Zhi] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.
[Liu, Yun-Mei] Univ South China, Inst Pharm Pharmacol, Hengyang 421001, Peoples R China.
[Song, Jian-Xin] Hunan Normal Univ, Key Lab Assembly & Applicat Organ Funct Mol Hunan, Changsha 410081, Hunan, Peoples R China.
通讯机构:
[Liu, Yun-Mei] U
[Song, Jian-Xin] H
Univ South China, Inst Pharm Pharmacol, Hengyang 421001, Peoples R China.
Hunan Normal Univ, Key Lab Assembly & Applicat Organ Funct Mol Hunan, Changsha 410081, Hunan, Peoples R China.
语种:
英文
关键词:
Chrysin derivatives;amino acid;anticancer;apoptotic
期刊:
亚洲天然物产研究(英文版)
ISSN:
1028-6020
年:
2020
卷:
22
期:
6
页码:
547-561
基金类别:
Hunan Natural Science FoundationNatural Science Foundation of Hunan Province [2018JJ2349]; University of South China Students Research Learning and Innovative Experimental Project [2018147200]
机构署名:
本校为通讯机构
院系归属:
药学与生物科学学院
摘要:
Amino acid derivatives containing chrysin were synthesized for evaluating their anticancer effects. Among them, compound N-(7-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)heptanoyl)-L-isoleucine (6e) displayed the most potent antiproliferative activity against MGC-803 cells with IC50 value of 20.0M. Preliminary mechanistic studies showed that compound 6e could inhibit the colony formation and migration of MGC-803 cells. Flow cytometry analysis demonstrated that compound 6e mediated cell apoptosis of MGC-803 cells and arrested cell cycle in G2/M-phase. Moreover, 6e treatment in MGC-803 cells ...

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