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- Title
Synthesis and Anti-HIV Activity of a Series of 6-Modified 2′,3′-Dideoxyguanosine and 2′,3′-Didehydro-2′,3′-dideoxyguanosine Analogs.
- Authors
Xie, Lujia; Yang, Xiantao; Pan, Delin; Cao, Yingli; Cao, Mou; Lin, Guichun; Guan, Zhu; Guo, Ying; Zhang, Lihe; Yang, Zhenjun
- Abstract
In search of potential 2′,3′-dideoxyguanosine (ddG) and 2′,3′-didehydro-2′,3′-dideoxyguanosine (D4G) prodrugs, a series of 6-modified ddG, D4G analogs were synthesized and evaluated for their anti-HIV activities and cytotoxities in cell-based assays. All analogs showed low cytotoxicities and some of them displayed benign anti-HIV activities. The active triphosphate forms in vivo, ddGTP and D4TTP, were also synthesized by a novel and facile "one-pot" method. The recognition of ddGTP and D4TTP by Taq, Therminater DNA polymerase and HIV reverse transcriptase (RT) incorporated in DNA/RNA strands were investigated by a non-radioactivity method and Km were determined.
- Subjects
GUANOSINE; ANTI-HIV agents; CELLS; RNA; DNA
- Publication
Chinese Journal of Chemistry, 2013, Vol 31, Issue 9, p1207
- ISSN
1001-604X
- Publication type
Article
- DOI
10.1002/cjoc.201300440