【摘要】 目的寻找具有抗肿瘤活性的新化合物,设计合成[1,2,4]三氮唑并[1,5-a]嘧啶衍生物,并评价其体外抗肿瘤活性。方法以γ-丁内酯为起始原料,经环合、氯代、取代、硫醚化和氨甲基化等反应合成7-苯基氨基-2-[3-(5-取代氨基甲基-呋喃-2-基-甲硫基)丙基]-5-甲基-[1,2,4]三氮唑并[1,5-a]嘧啶类化合物。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了评价。结果与结论合成了12个未见文献报道的新化合物,结构经质谱、红外光谱和核磁共振氢谱确证。体外活性实验表明:化合物16显示出很好的抗肿瘤活性。更多还原

【Abstract】 Aim To discovery novel compounds of antitumor activities,a series of [1,2,4]triazolo[1,5-a]pyrimidine derivatives were designed and synthesized.Methods Starting with γ-butyrolactone,followed by cyclization,chlorination,substitution,etherification,and aminomethylation,7-anilino-5-methyl-2-(3-((5-(substituted-aminomethyl)furan-2-yl)methylthio)propyl)[1,2,4]triazolo[1,5-a]pyramidine type of compounds were synthesized and their antitumor activities were evaluated with Bel-7402 and HT-1080 in vitro using cisplatin as control.Results and conclusion Twelve novel compounds were synthesized,and their structures were confirmed by 1H-NMR and MS.The in vitro antitumor activity showed that compound 16 displayed good antitumor activity.更多还原