Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.
- Published Article
Bioorganic & Medicinal Chemistry Letters
- Publication Date
Jan 20, 1998
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.
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The corresponding record at NLM can be accessed at https://www.ncbi.nlm.nih.gov/pubmed/9871653