Abstract
New 5′-alkyl ethoxy- and aminocarbonylphosphonates of 3′-azido-3′-deoxythymidine (AZT) were synthesized, and their antiviral properties in HIV-1-infected cell cultures and stability to chemical hydrolysis were studied. The AZT 5′-aminocarbonylphosphonates were shown to be significantly more stable in phosphate buffer (pH 7.2) than the corresponding ethoxycarbonylphosphonates. The therapeutic (selectivity) index of some of the compounds exceeded that of the parent AZT due to their higher antiviral activity.
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Shirokova, E.A., Jasko, M.V., Khandazhinskaya, A.L. et al. New Phosphonoformic Acid Derivatives of 3′-Azido-3′-Deoxythymidine. Russian Journal of Bioorganic Chemistry 30, 242–249 (2004). https://doi.org/10.1023/B:RUBI.0000030131.37092.0a
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DOI: https://doi.org/10.1023/B:RUBI.0000030131.37092.0a