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ID: ALA3734728
Journal: Bioorg Med Chem Lett
Title: 2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists.
Authors: Neochoritis CG, Wang K, Estrada-Ortiz N, Herdtweck E, Kubica K, Twarda A, Zak KM, Holak TA, Dömling A.
Abstract: The protein–protein interaction of p53 and MDM2/X is a promising non genotoxic anticancer target. A rapid and efficient methodology was developed to synthesize the 2,30-bis(10H-indole) heterocyclic scaffold 2 as ester, acid and amide derivatives. Their binding affinity with MDM2 was evaluated using both fluorescence polarization (FP) assay and HSQC experiments, indicating good inhibition and a perfect starting point for further optimizations.
CiteXplore: 26584879