Synthesis and Antitumor Activity Evaluation of Some Novel Pyrazolotriazine Derivatives

6-Aminopyrazolo[1,2-a][1,2,4]triazine-4,8-dione derivative <b>3</b> was obtained upon the reaction of the acid hydrazide derivative <b>2a</b> with ethyl cyanoacetate. The reactions of <b>3</b> with several electrophiles such as aldehydes, isatin, acetic anhydride, phenyl isocyanate, benzoyl isothiocyanate and p-toluenesulphonyl chloride were studied. The structures of the newly synthesized compounds were established on the basis of IR, ¹H-NMR, mass spectra, and elemental analyses. The antitumor activities of some selective compounds were examined against two cell lines as liver carcinoma cell line (HEPG-2) and human breast cancer cell line (MCF7).

将酰肼衍生物**2a**与氰乙酸乙酯进行反应，可得到6-氨基吡唑并[1,2-a][1,2,4]三嗪-4,8-二酮衍生物**3**。本研究考察了衍生物**3**与多种亲电试剂的反应，所涉亲电试剂包括醛类、靛红、乙酸酐、异氰酸苯酯、苯甲酰异硫氰酸酯及对甲苯磺酰氯。新合成化合物的结构通过红外光谱（IR）、氢核磁共振谱（¹H-NMR）、质谱及元素分析得以确证。选取部分化合物，针对肝癌细胞系（HEPG-2）与人乳腺癌细胞系（MCF7）两种细胞系开展了抗肿瘤活性测试。