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ID: ALA1138098

Journal: Bioorg Med Chem Lett

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

Authors: Leonard K, Marugan JJ, Raboisson P, Calvo R, Gushue JM, Koblish HK, Lattanze J, Zhao S, Cummings MD, Player MR, Maroney AC, Lu T.

Abstract: 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.

CiteXplore: 16647257

DOI: 10.1016/j.bmcl.2006.04.009