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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 synthesize 2 ’, 3’-open-loop 2’-3’-bisazide acyclic nucleosides and test their antiviral and antitumor activity in vitro. Methods: Natural nucleosides were used as starting materials to synthesize 4 kinds of azido acyclic nucleosides by NaN3 nucleophilic substitution after 2 ’, 3’-hydroxysulfonylation. RESULTS AND CONCLUSION: The four compounds synthesized were confirmed by 1HNMR, 13CNMR and HRMS. The preliminary bioassay showed that the compound has certain anti-HSV-I activity and no anti-T47D and NCI-H460 tumor cell activity. This result is helpful to further study the structure-activity relationship of these compounds.