新型O^6-苄基鸟嘌呤衍生物的合成及其细胞毒性

Synthesis and Cytotoxicity of A Novel O^6-benzylguanine Derivative

以O^6-苄基鸟嘌呤(O^6-BG)为起始原料,经4步反应合成了一个新型的O^6-BG衍生物——4-硝基苄基-[6-(苄氧基)-9H-嘌呤-2]氨基甲酸酯(4),其结构经1H NMR和HR-ESI-MS表征。用CCK-8法研究了4对人脑神经胶质细胞(SF126,SF763和SF767)的细胞毒性。结果表明:在低氧环境下,4与ACUN的协同作用对SF126,SF763和SF767均有较好的抑制活性,其IC50分别为0.04 m M,0.1 m M和0.03 m M,优于阳性对照药O^6-BG。

A novel O^6-benzylguanine( O^6-BG) derivative,4-nitrobenzyl-[6-( benzyloxy)-9H-purin-2-yl]carbamate( 4),was synthesized by a four-step reaction,using O^6-BG as starting material. The structure was characterized by1 H NMR and HR-ESI-MS. The cytotoxicities of 4 were investigated by CCK-8 method. The results indicated that 4 exhibited better inhibition activities against human glioma cell lines( SF126,SF763 and SF767) with ACUN than O^6-BG under hypoxia conditions. IC50 of 4 against SF126,SF763 and SF767 were 0. 04 m M,0. 1 m M and 0. 03 m M,respectively.