Design, synthesis, and preliminary biological evaluation of novel ethyl 1-(2′-hydroxy-3′-aroxypropyl)-3-aryl-1H-pyrazole-5-carboxylate

被引：122

作者：

Wei, Fang

Zhao, Bao-Xiang ^{[1
]}

Huang, Bin

Zhang, Lu

Sun, Chun-Hui

Dong, Wen-Liang

Shin, Dong-Soo

Miao, Jun-Ying

机构：

[1] Shandong Univ, Inst Organ Chem, Sch Chem & Chem Engn, Jinan 250100, Peoples R China

[2] Shandong Univ, Inst Dev Biol, Sch Life Sci, Jinan 250100, Peoples R China

[3] Changwon Natl Univ, Dept Chem, Chang Won 641773, South Korea

[4] Changwon Natl Univ, Res Inst Nat Sci, Chang Won 641773, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 24期

关键词：

pyrazole derivatives; A549; cells; growth inhibition;

D O I：

10.1016/j.bmcl.2006.09.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We synthesized a series of novel small molecules, ethyl 1-(2'-hydroxy-3'-aroxypropyl)-3-aryl-1H-pyrazole-5-carboxylate derivatives 3a-3o, by the reaction of ethyl 3-aryl-1H-pyrazole-5-carboxylate with 2-aryloxymethylepoxide in the presence of potassium carbonate at refluxing in acetonitrile in moderate or excellent yields. We investigated the effects of all the compounds on A549 cell growth. The results showed that 15 compounds could suppress A549 lung cancer cell growth. Among them, compound 3i was the most effective small molecule in inhibiting A549 cell growth. Compound 3f might most effectively induce A549 cell differentiation. Compound 3g remarkably induced cellular vacuolation. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：6342 / 6347

页数：6

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