Synthesis, anti-HIV, and cytotoxic activity of new AZT conjugates of steroid acids

In an attempt to discover potent anti-HIV agents devoid of the serious toxicity of the current HIV-reverse transcriptase inhibitors, three steroid prodrugs of AZT have been synthesized and their anti-HIV profiles determined with CEM-SS cell line. Two of the prodrugs were active against HIV, though weaker than AZT. The third agent was totally inactive against HIV. However, it demonstrated remarkably high anti-growth activities. Further experiments established that growth inhibition of the third agent was caused by induction of apoptosis rather than general necrosis.