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  • Title: Synthesis and anti-HIV activity of steroidal prodrugs of 3'-azido-3'-deoxythymidine (AZT).
    Author: Balagopala MI, Ollapally AP, Lee HJ.
    Journal: Cell Mol Biol (Noisy-le-grand); 1995; 41 Suppl 1():S1-7. PubMed ID: 8574137.
    Abstract:
    A total of seven steroidal prodrugs of AZT were synthesized and tested in vitro for their anti-HIV activity. Three of them were steroidal carboxylic esters prepared from steroidal 17 beta-carboxylic acids and AZT. The remaining four were alkyl steroidal phospho-triesters of AZT. These prodrugs were synthesized using known procedures. Preliminary results of in vitro anti-HIV activity screening showed that all of these prodrugs were active against HIV. While carboxylic esters showed comparable anti-HIV activity to that of AZT, phosphotriesters were less active than AZT. The therapeutic indices of all these prodrugs are comparable to that of AZT.
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