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  • Title: Design, synthesis, and evaluation of indole compounds as novel inhibitors targeting Gp41.
    Author: Zhou G, Wu D, Hermel E, Balogh E, Gochin M.
    Journal: Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1500-3. PubMed ID: 20153190.
    Abstract:
    A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant of compound 7 was 2.1microM, and the IC(50) for cell-cell fusion inhibition was 1.1microM. Assay data indicated that 7 is a promising lead compound for optimization into an effective low molecular weight fusion inhibitor.
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