In order to enhance the therapeutic efficacy of azidothymidine (AZT) by improving its pharmacokinetic properties, three prodrugs of AZT were synthesized by esterifying the 5′-hydroxyl of AZT with three pharmacologically inactive steroidal 17β-carboxylic acids. Preliminary results of in vitro anti-HIV activity screening of the compounds show that all of these esters have anti-HIV activity comparable to that of AZT. This report discusses the synthesis and anti-HIV activity screening results of the prodrugs.
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