1101861-36-2Relevant articles and documents
Design and synthesis of novel pyrazole-based Lp-PLA2 inhibitors
Wang, Yi,Xu, Weiren,Shao, Hua,Xie, Yafei,Wang, Jianwu
, p. 2039 - 2048 (2012/03/26)
A series of novel pyrazole-based lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitors have been designed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic approach is carefully opt
Synthesis and preliminary biological evaluation of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as potential agents against A549 lung cancer cells
Zhang, Jin-Hua,Fan, Chuan-Dong,Zhao, Bao-Xiang,Shin, Dong-Soo,Dong, Wen-Liang,Xie, Yong-Sheng,Miao, Jun-Ying
body text, p. 10165 - 10171 (2009/04/06)
A series of novel pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives were synthesized by the reaction of ethyl 3-aryl-1-(2-bromoethyl)-1H-pyrazole-5-carboxylate and amine in the general heating condition and microwave-assisted condition. The structures of the compounds were determined by IR, 1H NMR and mass spectroscopy, in addition, representative single-crystal structures were characterized by using X-ray diffraction analysis. Preliminary biological evaluation showed that the compounds could inhibit the growth of A549 cells in dosage- and time-dependent manners. The study on structure-activity relationships showed that compounds with 4-chlorophenyl group at pyrazole moiety, such as 5-benzyl-2-(4-chlorophenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one (3o) had much more inhibitory effects. Compound 3o was the most effective small molecule in inhibiting A549 cell growth and might perform its action through modulating autophagy.