Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents

被引：13

作者：

Xin, Ya-Bing ^{[1
]}

Li, Jia-Jun ^{[1
]}

Zhang, Hong-Jian ^{[1
]}

Ma, Jun ^{[2
]}

Liu, Xin ^{[1
]}

Gong, Guo-Hua ^{[3
,4
]}

Tian, Yu-Shun ^{[1
]}

机构：

[1] Yanbian Univ, Coll Pharm, Affiliated Minist Educ, Key Lab Nat Resources & Funct Mol Changbai Mt, Yanji 133002, Jilin, Peoples R China

[2] Jiangsu Hansoh Pharmaceut Grp Co Ltd, Lianyungang, Peoples R China

[3] Inner Mongolia Univ Nationalities, Clin Med Coll 1, Tongliao 028002, Inner Mongolia, Peoples R China

[4] Inner Mongolia Univ Nationalities, Inner Mongolia Key Lab Mongolian Med Pharmacol Ca, Tongliao, Peoples R China

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2018年 / 33卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Styrylbenzene; cyano; selective toxic effect; anticancer; synthesis; TUBULIN POLYMERIZATION INHIBITORS; IN-VITRO EVALUATION; BIOLOGICAL EVALUATION; ACID-DERIVATIVES; ANTIPROLIFERATIVE ACTIVITY; COMBRETASTATIN ANALOGS; DESIGN; 1,2,3-TRIAZOLE;

D O I：

10.1080/14756366.2018.1513925

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five cancer cell lines, including MGC-803 and BEL-7402. (Z)-3-(p-Tolyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile (6h) showed a strong inhibitory effect on MGC-803 cells (IC50<0.01 mu M) and exhibited stronger anti-proliferative activity than taxol (IC50<0.06 +/- 0.01 mu M). The IC50 value of 6h in L-02 cells was 10,000-fold higher than in MGC-803 cells. Compound 6h inhibited proliferation of BEL-7402 cells by arresting at the G2/M phase through up-regulation of cyclin B1 expression, down-regulation of cyclin A and D1 expression, and induction of apoptosis. In addition, 6h inhibited the migration of BEL-7402 cells and the formation of cell colonies.

引用

收藏

页码：1554 / 1564

页数：11

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