吡唑并[1，5-α]嘧啶类化合物的合成及其抗肿瘤活性

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。

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

Ai mTo design andsynthesize novel pyrazolo[1,5-a]pyri midine derivatives,andto assaytheir an-titumor activities.MethodsBased on the general structure of pyrazolo[1,5-a]pyri midine having antitumoractivity,5-aminomethyl-7-anilinopyrazolo[1,5-a] pyri midines were designed,and the target compoundswere synthesizedviaafive-step procedure startingfrom malononitrile andtriethyl orthoformate.Using cis-platin as positive control,their antitumor activities were evaluated with Bel-7402 and HT-1080in vitro.Re-sults and conclusionsEleven novel compounds were synthesized,andtheir structures were confirmed by1H-NMRand MS.Among them,compound6displayed good antitumor activity.