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- W2113102774 abstract "This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA approval of 5-azacytidine (Vidaza ® ) and 2´-deoxy-5-azacytidine (Dacogen ® ) for the treatment of myelodysplastic syndromes. 5,6-dihydro-2´-deoxy-5-azacytidine, a compound with anti-HIV activity through lethal mutagenesis, representing a unique mechanism of action among existing anti-retroviral drugs, is discussed together with quite recent discovery of its so far unexpected hypomethylation activity. Special attention is paid to 5-azacytosine acyclic nucleoside analogues and phosphonomethyl derivatives with the emphasis on the new potent anti-DNA virus agent (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine and its prodrug forms. Considering the potential pharmaceutical applications, 5-azacytosine and 5,6-dihydro-5-azacytosine appear to be so far the most effective cytosine mimics for the design of novel antiviral and anti-tumor drug candidates." @default.
- W2113102774 created "2016-06-24" @default.
- W2113102774 creator A5013206001 @default.
- W2113102774 creator A5024818475 @default.
- W2113102774 date "2012-05-01" @default.
- W2113102774 modified "2023-10-17" @default.
- W2113102774 title "5-azacytosine compounds in medicinal chemistry: current stage and future perspectives" @default.
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- W2113102774 doi "https://doi.org/10.4155/fmc.12.36" @default.
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