School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):844-9. doi: 10.1016/j.bmcl.2011.12.049. Epub 2011 Dec 16.
A series of substituted 5-benzyl-2-phenylpyrazolo[1,5-a]pyrazin-4,6(5H,7H)-dione derivatives was synthesized by one-step reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and N-arylalkyl-2-chloroacetamide. 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. The compound 5j could selectively inhibit the growth of H322 lung cancer cells which contain a mutated p53 gene in a dose-dependent manner through inducing apoptosis of cells.
一系列取代的 5-苄基-2-苯基吡唑并[1,5-a]吡嗪-4,6(5H,7H)-二酮衍生物是通过一步反应合成的，反应物为乙基 3-苯基-1H-吡唑-5-羧酸酯衍生物和 N-芳基烷基-2-氯乙酰胺。通过红外光谱（IR）、（1）H 核磁共振（NMR）和质谱（MS）确定了化合物的结构。此外，通过 X 射线衍射分析对代表性的单晶结构进行了表征。化合物 5j 能够通过诱导细胞凋亡，以剂量依赖的方式选择性地抑制含有突变 p53 基因的 H322 肺癌细胞的生长。
