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  • Title: Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.
    Author: Velanguparackel W, Hamon N, Balzarini J, McGuigan C, Westwell AD.
    Journal: Bioorg Med Chem Lett; 2014 May 15; 24(10):2240-3. PubMed ID: 24751439.
    Abstract:
    A series of pro-nucleotide phosphoramidates and phosphorodiamidates of the antiviral lead compound 3'-deoxy-3'-fluorothymidine (FLT) have been designed and synthesized. In vitro antiretroviral and cytostatic studies revealed potent (sub-micromolar) inhibition of HIV-1 and HIV-2 replication, with retention of activity in thymidine kinase-negative cell models, as predicted by the ProTide concept.
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