标题：Microwave-assisted synthesis, crystal structure of pyrazolo(1,5-a)pyrazin-4(5H)-ones and their selective effects on lung cancer cells.
作者：Liu N;Zhang JH;Zhao BX;Zhao J;Su L;Dong WL;Zhang SL;Miao JY
作者机构：[Liu, N] Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, School of Life Science, Shandong University, Jinan 250100, Chin 更多
通讯作者地址：[Zhao, BX]Shandong Univ, Inst Organ Chem, Sch Chem & Chem Engn, Jinan 250100, Peoples R China.
来源：European Journal of Medicinal Chemistry: Chimie Therapeutique
关键词：Pyrazole; Pyrazinone; Microwave-assisted synthesis; Single-crystal; Lung; cancer cells
摘要：A series of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives with hydrophilic group was synthesized under general heating condition and microwave-assisted condition. The structures of compounds were determined by IR, 1H NMR and HRMS, moreover, representative crystal structures were characterized by using X-ray diffraction analysis. Preliminary biological evaluation showed that some compounds could inhibit the growth of A549, H322 and H1299 cells in dosage dependent manners. The compounds could inhibit growth of A549, H322 and H1299 cells in different mechanism. Compounds 3e-h inhibited growth of A549 cells by inducing a strong G1-phase arrest. Whereas these compounds inhibited growth of H1299 and H322 cells by inducing apoptosis.