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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites
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Fluorescence Polarization
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / chemistry*
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Heterocyclic Compounds / metabolism
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Indoles / chemistry
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Molecular Docking Simulation
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Protein Interaction Domains and Motifs
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Protein Structure, Tertiary
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Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors*
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Proto-Oncogene Proteins c-mdm2 / metabolism
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Tumor Suppressor Protein p53 / antagonists & inhibitors*
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Tumor Suppressor Protein p53 / metabolism
Substances
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Heterocyclic Compounds
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Indoles
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Tumor Suppressor Protein p53
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indole
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Proto-Oncogene Proteins c-mdm2