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Synthesis of a Non-Nucleoside Reverse Transcriptase Inhibitor in the Alkenyldiarylmethane (Adam) Series With Optimized Potency and Therapeutic Index

  1. Author:
    Cushman, M.
    Casimirogarcia, A.
    Williamson, K.
    Rice, W. G.
    1. Year: 1998
  1. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 8
    2. 2
    3. Pages: 195-198
  2. Type of Article: Article
  1. 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-1(RF) in CEM-SS cells with an EC50 of 13 nM, while it shows cytotoxicity with a CC50 of 31.6 mu M, providing a therapeutic index of 2430. ADAM II is a non-nucleoside reverse transcriptase inhibitor, displaying an IC50 of 0.3 mu M with poly(rC) oligo(dG) as the template/primer. (C) 1998 Elsevier Science Ltd. All rights reserved. [References: 17]

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