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
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
收藏
页码:5325 / 5328
页数:4
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