Design and Synthesis of Novel Butenolide Derivatives and Inducing Apoptosis in Gastric Cancer Cells

被引：0

作者：

Xu, Haiwei ^{[1
]}

Li, Yuanyuan ^{[1
]}

Dong, Hangqi ^{[1
]}

Meng, Xia ^{[1
]}

Zhao, Lingjie ^{[1
]}

Lu, Chuntao ^{[1
]}

Wang, Zhenya ^{[1
]}

Jin, Chengyun ^{[1
]}

机构：

[1] Zhengzhou Univ, Key Lab Henan Prov Drug Qual Control & Evaluat, Collaborat Innovat Ctr New Drug Res & Safety Eval, Key Lab Drug Preparat Technol,Minist Educ,Sch Pha, Zhengzhou 450001, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 01期

关键词：

butenolide; synthesis; gastric cancer; apoptosis; caspase; IN-VITRO; DEATH;

D O I：

10.6023/cjoc201907018

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new method of preparation for natural product Uncinine was reported. According to the method, a series of novel butenolides derivatives were designed and synthesized based on the natural product Uncinine. Most of the synthetic compounds showed significant anti proliferation activity against MGC-803. Among of them, (Z)-5-(4-(tert-butyl)-benzylidene)-3-(morpholinomethyl)furan-2(5H)-one (9l) showed potent anticancer effect with IC50 of 2.9 mu mol/L in gastric cancer cell MGC803 and showed good selectivity to gastric cancer cells MGC803, HGC27, SGC7901 and less cytotoxicity in normal gastric epithelial cell line (GES1). The research on the molecular level suggests that the mechanism of compound 9l inducing apoptosis in gastric cancer cells is partially dependent on activation of caspase-9/3.

引用

页码：69 / 77

页数：9

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