Article
4'-Ethynylstavudine (4'-Ed4T) has potent anti-HIV-1 activity with reduced toxicity and shows a unique activity profile against drug-resistant mutants.
Antiviral chemistry & chemotherapy - 1 Jan 2005
Tanaka Hiromichi, Haraguchi Kazuhiro, Kumamoto Hiroki, Baba Masanori, Cheng Yung-Chi
Abstract excerpt
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...
Topics
- Anti-HIV Agents
- Cell Line
- DNA, Mitochondrial
- Drug Resistance, Viral
- HIV-1
- Humans
- Molecular Structure
- Mutation
- Stavudine
- Structure-Activity Relationship
- Substrate Specificity
- Thymidine Kinase
- Thymidine Phosphorylase