新型2,4-二羟基蝶啶类衍生物的合成及其抗肿瘤活性  

Synthesis and Antitumor Activity of Novel 2,4-Dihydroxypteridine Derivatives

作　　者：何欢 唐潇 王勉[2] 王坚毅[1,3] HE Huan;TANG Xiao;WANG Mian;WANG Jianyi(College of Chemistry and Chemical Engineering,Guangxi University,Nanning 530004,China;College of Life Science and Technology,Guangxi University,Nanning 530004,China;Medical College,Guangxi University,Nanning 530004,China)

机构地区：[1]广西大学化学化工学院,广西南宁530004 [2]广西大学生命与科学技术学院,广西南宁530004 [3]广西大学医学院,广西南宁530004

出　　处：《合成化学》2024年第3期209-215,224,共8页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21967003)。

摘　　要：蝶啶类化合物的抗肿瘤活性是研究最多,也是最具有治疗潜力的一类化合物。以Ibrutinib为先导化合物,以4-氨基-2,6-二羟基嘧啶为原料出发,经过多步首次合成了新型2,4-二羟基蝶啶类衍生物,并对其进行了^(1)H NMR、^(13)C NMR和MS(ESI)的表征。选用A549细胞做了抗肿瘤实验,结果表明:化合物5h,5j和6o在低浓度下表现出小于10%的抑制率,在高浓度下均有大于20%的抑制率,说明5h,5j和6o对A549细胞有一定的抑制效果。The antitumor activity of pteridine-based compounds is one of the most studied and advanced.In this article,Ibrutinib was used as the lead compound,starting from 4-amino-2,6-dihydroxypyrimidine,2,4-dihydroxypyternidine derivatives were synthesized and characterized by ^(1)H NMR,^(13)C NMR and MS(ESI).Using Ibrutinib as positive drug,A549 cells were selected for anti-tumor experiments.The results showed that compounds 5h,5j and 6o exhibited inhibition rates of less than 10%at low concentration and greater than 20%at high concentration,indicating that 5h,5j and 6o had certain inhibitory effects on A549 cells.

关 键 词：4-氨基-2 6-二羟基嘧啶 合成 蝶啶衍生物 A549 依鲁替尼 

分 类 号：O626[理学—有机化学]