Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity

The disruption of the p53-Hdm2 protein–protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.

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