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

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.