Phosphoramidate and phosphate prodrugs of (−)-β-d-(2R, 4R)-dioxolane-thymine: Synthesis, anti-HIV activity and stability studies

Y Liang, J Narayanasamy, RF Schinazi…

文献索引：Liang, Yuzeng; Narayanasamy, Janarthanan; Schinazi, Raymond F.; Chu, Chung K. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 7 p. 2178 - 2189

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被引用次数: 35

摘要

A series of phosphoramidate and phosphate prodrugs of DOT were synthesized via dichlorophosphate or H-phosphonate chemistry and evaluated for their anti-HIV activity against LAI M184V mutants in PBM cells as well as for their cytotoxicity. The antiviral and cytotoxic profiles of the prodrugs were compared with that of the parent compound (DOT), and it was found that four aryl phosphoramidates 5, 18, 20, and 26 showed a significant ...