抗肿瘤化合物L-5'-noraristeromycin类似物的设计与合成

抗肿瘤化合物L-5'-noraristeromycin类似物的设计与合成

黄民俊, 杨振军, 张亮仁^*, 张礼和

北京大学天然药物及仿生药物国家重点实验室, 北京 100191

收稿日期:2009-06-20 修回日期:2009-10-15 出版日期:2009-11-30 发布日期:2009-11-30
通讯作者: 张亮仁*

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

Min-Jun Huang, Zhen-Jun Yang, Liang-Ren Zhang^*, Li-He Zhang

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

Received:2009-06-20 Revised:2009-10-15 Online:2009-11-30 Published:2009-11-30
Contact: Liang-Ren Zhang*

摘要/Abstract

摘要： 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: 碳环核苷, L-核苷类似物, 抗肿瘤

Abstract:

Nucleoside analogues show a variety of biological activities. To prepare new purine nucleoside analogues that could inhibit the proliferation of tumor cells and resist enzyme 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.

Key words: Carbocyclic nucleoside, L-Nucleoside analogue, Antitumor

中图分类号:

R916.4

Supporting: Foundation item: National Natural Science Foundation of China (Grant No. 20672010).

^*Corresponding author. Tel.: 86-10-82802567; e-mail: liangren@bjmu.edu.cn

黄民俊, 杨振军, 张亮仁^*, 张礼和. 抗肿瘤化合物L-5'-noraristeromycin类似物的设计与合成[J]. .

Min-Jun Huang, Zhen-Jun Yang, Liang-Ren Zhang^*, Li-He Zhang . Design and synthesis of L-5'-noraristeromycin analogues as potent antitumor agents [J]. .

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