Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells

被引：47

作者：

Ding, Xiao-Ling ^{[1
,3
]}

Zhang, Hai-Yan ^{[2
]}

Qi, Lei ^{[2
]}

Zhao, Bao-Xiang ^{[1
]}

Lian, Song ^{[1
]}

Lv, Hong-Shui ^{[1
]}

Miao, Jun-Ying ^{[2
]}

机构：

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

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

[3] Qingdao Univ, Coll Adv Profess Technol, Qingdao 266061, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 18期

基金：

中国国家自然科学基金;

关键词：

Pyrazole; Carboxamide; A549; cells; Apoptosis; Autophagy; BIOLOGICAL EVALUATION; RECEPTOR ANTAGONISTS; POTENTIAL AGENTS; DESIGN; INHIBITORS;

D O I：

10.1016/j.bmcl.2009.07.131

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 3-aryl-1-arylmethyl-1H-pyrazole-5-carboxamide derivatives 3a-1, were synthesized by the reaction of 3-aryl-1-arylmethyl-1H-pyrazole-5-carbonyl chloride with substituted amine in excellent yields. The compounds 3e-h could suppress A549 lung cancer cell growth, More interestingly, compounds 3e and 3f might inhibit the A549 cell growth by inducing apoptosis; whereas compounds 3g and 3h with fluorine group might inhibit the A549 cell growth by inducing autophagy. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5325 / 5328

页数：4

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