叠氮无环核苷的制备、表征及活性测试  

Preparation,characterization and biological evaluation of azido-seconucleoside analogues

作　　者：冉旭[1] 白永[2] 陈尧[1,2] 姜发琴[1] 张健存[3] 傅磊[1] 

机构地区：[1]上海交通大学药学院,上海200240 [2]石药集团新诺威制药股份有限公司,石家庄051430 [3]中国科学院广州生物医药与健康研究院,广州510663

出　　处：《中国新药杂志》2009年第20期1995-1998,2001,共5页Chinese Journal of New Drugs

基　　金：上海市科委重大科技项目(04DZ19209);上海市教育委员会科研创新项目(08ZZ12)

摘　　要：目的:合成2’,3’-开环-2’-3’-双叠氮无环核苷化合物,并测试其体外抗病毒及抗肿瘤活性。方法:以天然核苷为原料,对2’,3’-羟基磺酰化后,通过NaN3亲核取代,合成4种叠氮基无环核苷化合物。结果与结论:合成的4种化合物经由1HNMR,13CNMR和HRMS确证。初步生物活性测试证明化合物具有一定抗HSV-I病毒活性,无抗T47D和NCI-H460肿瘤细胞活性,此结果为进一步研究该类化合物构效关系提供了帮助。Objective：To synthetize 2’,3’-azido-2’,3’-seconucleoside analogues,and to determine the potential antiviral activity.Methods：The target compounds were synthesized from natural nucleosides,through sulfonylation at 2’,3’-OH and nucleophilic substitution by NaN3.Results and Conclusion：The structures of these compounds were confirmed by 1H NMR,13C NMR and HRMS analyses.All the target compounds showed moderate anti-HSV-I activity,which might contribute to the research on SAR of nucleosides analogues in this field.

关 键 词：叠氮基 无环核苷 制备 表征 活性 

分 类 号：R978.7[医药卫生—药品] R979.1[医药卫生—药学]