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  • Title: Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction.
    Author: Vaupel A, Bold G, De Pover A, Stachyra-Valat T, Lisztwan JH, Kallen J, Masuya K, Furet P.
    Journal: Bioorg Med Chem Lett; 2014 May 01; 24(9):2110-4. PubMed ID: 24704029.
    Abstract:
    Capitalizing on crystal structure information obtained from a previous effort in the search for non peptide inhibitors of the p53-MDM2 interaction, we have discovered another new class of compounds able to disrupt this protein-protein interaction, an important target in oncology drug research. The new inhibitors, based on a tetra-substituted imidazole scaffold, have been optimized to low nanomolar potency in a biochemical assay following a structure-guided approach. An appropriate strategy has allowed us to translate the high biochemical potency in significant anti-proliferative activity on a p53-dependent MDM2 amplified cell line.
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