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. 2006 Jul 1;16(13):3463-8.
doi: 10.1016/j.bmcl.2006.04.009. Epub 2006 May 2.

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

Kristi Leonard  1 , Juan Jose Marugan, Pierre Raboisson, Raul Calvo, Joan M Gushue, Holly K Koblish, Jennifer Lattanze, Shuyuan Zhao, Maxwell D Cummings, Mark R Player, Anna C Maroney, Tianbao Lu
Affiliations

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

Kristi Leonard et al. Bioorg Med Chem Lett. .

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.

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