目的设计合成新的吡唑并[1,5-a]嘧啶类化合物,并评价其抗肿瘤活性。方法根据吡唑并[1,5-a]嘧啶类抗肿瘤药物的基本结构设计了一系列5-胺甲基-7-苯胺基吡唑并[1,5-a]嘧啶类化合物,并以丙二腈和原甲酸三乙酯为起始原料,经5步反应得到目标产物。采用MTT法,以顺铂为阳性对照药,以Bel-7402和HT-1080为测试细胞株对目标化合物的抗肿瘤活性进行评价。结果与结论合成了11个未见文献报道的化合物,结构经质谱和核磁共振氢谱确证。化合物6显示出很好的抗肿瘤活性。 Aim To design and synthesize new pyrazolo [1,5-a] pyrimidines and evaluate their antitumor activity. Methods A series of 5-aminomethyl-7-anilino-pyrazolo [1,5-a] pyrimidines were designed according to the basic structure of pyrazolo [1,5-a] Malononitrile and triethyl orthoformate as starting materials, the target product was obtained after 5 steps. The antitumor activity of the target compounds was evaluated by MTT assay with cisplatin as positive control and Bel-7402 and HT-1080 as test cell lines. RESULTS AND CONCLUSIONS Eleven compounds that were not reported in the literature were synthesized and their structures were confirmed by MS and 1H NMR. Compound 6 shows good anti-tumor activity.