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. 2005 Feb 1;15(3):765-70.
doi: 10.1016/j.bmcl.2004.11.009.

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR

Daniel J Parks  1 , Louis V Lafrance, Raul R Calvo, Karen L Milkiewicz, Varsha Gupta, Jennifer Lattanze, Kannan Ramachandren, Theodore E Carver, Eugene C Petrella, Maxwell D Cummings, Diane Maguire, Bruce L Grasberger, Tianbao Lu
Affiliations

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR

Daniel J Parks et al. Bioorg Med Chem Lett. .

Abstract

A library of 1,4-benzodiazepine-2,5-diones was screened for binding to the p53-binding domain of HDM2 using Thermofluor, a miniaturized thermal denaturation assay. The hits obtained were shown to bind to HDM2 in the p53-binding pocket using a fluorescence polarization (FP) peptide displacement assay. The potency of the series was optimized, leading to sub-micromolar antagonists of the p53-HDM2 interaction.

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