Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, School of Life Science, Shandong University, Jinan 250100, PR China.
Eur J Med Chem. 2011 Jun;46(6):2359-67. doi: 10.1016/j.ejmech.2011.03.018. Epub 2011 Mar 15.
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.
在常规加热条件和微波辅助条件下，合成了一系列带有亲水基团的新型吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物。通过红外光谱（IR）、1H 核磁共振（1H NMR）和高分辨质谱（HRMS）确定了化合物的结构，此外，还通过 X 射线衍射分析对代表性晶体结构进行了表征。初步的生物评价表明，部分化合物能够以剂量依赖的方式抑制 A549、H322 和 H1299 细胞的生长。这些化合物通过不同的机制抑制 A549、H322 和 H1299 细胞的生长。化合物 3e-h 通过诱导强烈的 G1 期阻滞来抑制 A549 细胞的生长。而这些化合物通过诱导细胞凋亡来抑制 H1299 和 H322 细胞的生长。
