Synthesis and Antitumor Activity of Novel 2,4-Dihydroxypteridine Derivatives
何欢 1唐潇 2王勉 2王坚毅3
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作者信息
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 化学化工学院,广西 南宁 530004;广西大学 医学院,广西 南宁 530004
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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.
Abstract
The antitumor activity of pteridine-based compounds is one of the most studied and ad-vanced.In this article,Ibrutinib was used as the lead compound,starting from 4-amino-2,6-di-hydroxypyrimidine,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 an-ti-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.
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