5,7-二取代吡唑并[1,5-a]嘧啶类化合物的合成及其抗肿瘤活性

Synthesis and antitumor activities of 5,7-disubstituted pyrazolo[1,5-a]pyrimidines

目的设计并合成吡唑并[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14个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,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进行抗肿瘤活性评价。结果与结论合成了14个未见文献报道的新化合物,结构经MS、IR和1H-NMR确证。体外活性实验表明:化合物12显示出较好的抗癌活性。

Aim To design and synthesize novel pyrazolo[ 1, 5-α ] pyrimidine derivatives, and to assay their antitumor activities. Methods Based on the general structure of pyrazolo[ 1,5-α ] pyrimidine processing antitumor activity, 5-amino-7-anilinopyrazol [ 1, 5-α ] pyrimidines were designed, and the target compounds were synthesized v/a a five-step procedure starting from malononitrile and triethyl orthoformate. Using cisplatin as control, the antitumor activities was evaluated against Bel-7402 and HT-1080 in vitro. Results and eonelusion Fourteen novel compounds were synthesized, and their structures were confirmed by 1H- NMR, IR and MS. Among them, compound 12 displayed good antitumor activities.