Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.
- Authors
- Type
- Published Article
- Journal
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier
- Publication Date
- Jan 20, 1998
- Volume
- 8
- Issue
- 2
- Pages
- 195–198
- Identifiers
- PMID: 9871653
- Source
- Medline
- License
- Unknown
Abstract
A novel alkenyldiarylmethane (ADAM) analog has been synthesized with enhanced potency as an anti-HIV agent. The new compound (ADAM II) inhibits the cytopathic effect of HIV-1RF in CEM-SS cells with an EC50 of 13 nM, while it shows cytotoxicity with a CC50 of 31.6 microM, providing a therapeutic index of 2430. ADAM II is a non-nucleoside reverse transcriptase inhibitor, displaying an IC50 of 0.3 microM with poly(rC) oligo(dG) as the template/primer.
