Synthesis of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives and their inhibition against growth of A549 and H322 lung cancer cells

被引：30
作者：
Zheng, Liang-Wen [1 ]
Shao, Jin-Hui [2 ]
Zhao, Bao-Xiang [1 ]
Miao, Jun-Ying [2 ]
机构：
[1] Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China
[2] Shandong Univ, Sch Life Sci, Jinan 250100, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 13期
基金：
中国国家自然科学基金;
关键词：
Synthesis; Microwave-assisted; Pyrazinone; X-ray; A549; cells; H322; PRELIMINARY BIOLOGICAL EVALUATION; SINGLE-CRYSTAL CHARACTERIZATION; MICROWAVE-ASSISTED SYNTHESIS; ANTITUMOR-ACTIVITY; ORGANIC-SYNTHESIS; ANTICANCER; AGENTS; PYRAZOLES; ASSAY;
D O I：
10.1016/j.bmcl.2011.05.035
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted pyrazolo[1,5-a]pyrazin-4(5H)-one was synthesized by the reaction of ethyl 1-(2-oxo-2-phenylethyl)-3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-(2-aminoethoxy) ethanol or 2-morpholinoethanamine in the condition of microwave-assisted one-step and solvent-free in a good yield. The structures of the compounds were determined by IR, (1)H NMR and mass spectroscopy. In addition, a representative single-crystal structure was characterized by using X-ray diffraction analysis. Preliminary biological evaluation showed that the compounds could inhibit the growth of A549 and H322 cells in dosage-dependent manners. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3909 / 3913
页数：5
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