Free accessResearch articleFirst published online 2005-8
Pointer 4'-Ethynylstavudine (4'-Ed4T) Has Potent Anti-HIV-1 Activity with Reduced Toxicity and Shows a Unique Activity Profile against Drug-Resistant Mutants
A nucleoside analogue 4'-ethynylstavudine (4'-Ed4T) was recently synthesized during chemical studies directed towards the development of a new route to 4' -carbon-substituted nucleosides. This compound was found to be more anti-HIV-1 active than the parent compound stavudine (d4T) and much less toxic to various cells and also to mitochondrial DNA synthesis. It became apparent that 4' -Ed4T is a better substrate for human thymidine kinase than d4T, and very much more resistant to catabolism by thymidine phosphorylase. The study of 4' -Ed4T against various drug-resistant HIV-1 mutants has disclosed its unique activity profile.
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