Design, synthesis and bioevaluation of novel prenylated chalcones derivatives as potential antitumor agents

被引：3

作者：

Yu, Jia ^{[1
,2
]}

Wang, Xia ^{[1
,2
,3
]}

Cheng, Sha ^{[1
,2
]}

Zeng, Xiaoping ^{[1
,2
]}

Wan, Xinwei ^{[1
,2
]}

Wei, Shinan ^{[1
,2
]}

Xu, Bixue ^{[1
,2
]}

Luo, Heng ^{[1
,2
]}

Meng, Xueling ^{[1
,2
]}

机构：

[1] Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China

[2] Nat Prod Res Ctr Guizhou Prov, Guiyang 550014, Peoples R China

[3] Suiyang Cty Hosp Tradit Chinese Med, Suiyang 563300, Peoples R China

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2024年 / 192卷

关键词：

Prenylated chalcone derivatives; Antitumor; Cytotoxicity; PI3K/AKT pathway; ANTICANCER; PROLIFERATION; APOPTOSIS; PRODUCTS; ANALOGS; CELLS;

D O I：

10.1016/j.ejps.2023.106660

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of novel prenylated chalcone derivatives with broad spectrum anticancer potential were designed and synthesized. Some of the synthesized target compounds showed potent anti-proliferative activities toward LNCaP (prostate cancer cell line), K562 (human leukemia cells), A549 (human lung carcinoma cell line) and HeLa (cervical cancer cell line) cell lines. Among of the active compounds, (E)-1-(4-(2-(diethylamino)ethoxy)-2-hy-droxy-6-methoxy-3-(3-methylbut-2-en-1-yl)phenyl)-3-(pyridin-3-yl)prop-2-en-1-one (C36) was directly inter-acted with protein kinase B (PKB), also known as AKT, significantly inhibited the pPI3K, pAKT(Ser473) protein levels to repress the growth of cancer cells by inducing apoptosis, arresting cell cycle. Our studies provide support for prenylated chalcone derivatives potential applications in cancer treatment as a potential AKT inhibitor.

引用

页数：15

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