2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists.

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.

SUBMITTER: Neochoritis CG 

PROVIDER: S-EPMC4764400 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature