Synthesis and Anti-HIV Activity of a Series of 6-Modified 2',3'-Dideoxyguanosine and 2',3'-Didehydro-2',3'- dideoxyguanosine Analogs

查看全文 作　　者：Lujia [1]Xie;Xiantao [1]Yang;Delin [1]Pan;Yingli [2]Cao;Mou [1]Cao;Guichun [1]Lin;Zhu [1]Guan;Ying [2]Guo;Lihe [1]Zhang;Zhenjun [1]Yang

机构地区：[1]State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China;[2]Institute ofMateria Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

出　　处：《Chinese Journal of Chemistry》索引2013年第31卷第9期,共12页

基　　金：The research was supported by the fund of the National Natural Science Foundation of China,the Ministry of Science and Technology of China (No.2008ZX10303).Anti-HIV activity evaluation in pseudotyped HIV system was performed by Institute of Materia Medica,Chinese Academy of Medical Science and Peking Union Medical College.Anti-HIV activity evaluation in HIV-1/MT2 cells was performed by HD 摘　　要：寻找潜在的 2,3-dideoxyguanosine (ddG ) 和 2,3-didehydro-2,3-dideoxyguanosine (D4G ) prodrugs,一系列 6-modified ddG, D4G 类似物在基于房间的试金为他们的 anti-HIV 活动和 cytotoxities 被综合并且评估。所有类似物显示出低 cytotoxicities,他们中的一些显示了良性的 anti-HIV 活动。在 vivo, ddGTP 和 D4TTP 的活跃 triphosphate 形式,被一个新奇、灵巧的“一个壶”也综合方法。由 Taq, Therminater DNA 聚合酶和在 DNA/RNA 海滨合并的 HIV 反向的 transcriptase (RT ) 的 ddGTP 和 D4TTP 的识别被一个非放射性方法调查, Km 是坚定的。 关键词：抗HIV活性类似物脱氧合成改性脱氢 DNA聚合酶 Taq酶

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Synthesis and Anti-HIV Activity of a Series of 6-Modified 2',3'-Dideoxyguanosine and 2',3'-Didehydro-2',3'- dideoxyguanosine Analogs

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