2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents

被引：31

作者：

Gao, Hui ^{[1
]}

Zhang, Xia ^{[1
]}

Pu, Xiao-Jia ^{[1
]}

Zheng, Xi ^{[2
]}

Liu, Bei ^{[1
]}

Rao, Gao-Xiong ^{[1
]}

Wan, Chun-Ping ^{[2
]}

Mao, Ze-Wei ^{[1
]}

机构：

[1] Yunnan Univ Tradit Chinese Med, Coll Pharmaceut Sci, Kunming 650500, Yunnan, Peoples R China

[2] Yunnan Univ Tradit Chinese Med, Affiliated Hosp 1, Cent Lab, Kunming 650021, Yunnan, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 06期

关键词：

2-Benzoylbenzofuran; Anticancer activity; Cytotoxicity; Apoptosis; HYBRID COMPOUNDS; DESIGN; BENZOFURAN;

D O I：

10.1016/j.bmcl.2019.01.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-benzoylbenzofuran derivatives possessing piperazine linker have been prepared, and their in vitro anticancer activity against a panel of human tumor cell lines by MTT assay were evaluated. The results demonstrated that tertiary amine derivatives exhibited better cytotoxic activity, and SAR study revealed that electron-donating substituents on the phenyl ring of the derivatization functionality contributed to potent anticancer activities. Among them, compounds 6, 9, 11, 18, 23 and 25 displayed both better anti-tumor activity and lower cytotoxic effect on human normal liver cell L02. Further apoptosis analysis showed that compound 18 significantly induced apoptosis in A549 cell, which was considered as the most potent anticancer agent.

引用

页码：806 / 810

页数：5

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