Design and synthesis of L-5'-noraristeromycin analogues as potent antitumor agents  

抗肿瘤化合物L-5'-noraristeromycin类似物的设计与合成(英文)

作　　者：黄民俊[1] 杨振军[1] 张亮仁[1] 张礼和[1] 

机构地区：[1]北京大学天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2009年第4期313-319,共7页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.20672010)

摘　　要：Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyrne hydrolysis, we designed and synthesized 15 different L-5＇noraristeromycin analogues, in which thioether, sulfoxide or sulfone function was introduced to replace the 5＇-hydroxymethyl group. Their anti-tumor activities were assayed in vitro. One compound showed potent anti-tumor activity.核苷类似物显示了广泛的生物活性。为了寻找具有抗肿瘤活性并同时具有酶稳定性的嘌呤化合物,我们在L-5′-noraristeromycin的5′-位分别引入硫醚、砜、亚砜基团,设计并合成了15个L-5′-noraristeromycin类似物,并测试了这些化合物的体外抗肿瘤活性。一个化合物显示了对肿瘤细胞具有较强抑制活性。

关 键 词：Carbocyclic nucleoside L-Nucleoside analogue ANTITUMOR 

分 类 号：R914[医药卫生—药物化学]