Enantiomerically pure 1, 4-benzodiazepine-2, 5-diones as Hdm2 antagonists

…, K Leonard, P Raboisson, JM Gushue, R Calvo…

文献索引：Marugan, Juan Jose; Leonard, Kristi; Raboisson, Pierre; Gushue, Joan M.; Calvo, Raul; Koblish, Holly K.; Lattanze, Jennifer; Zhao, Shuyuan; Cummings, Maxwell D.; Player, Mark R.; Schubert, Carsten; Maroney, Anna C.; Lu, Tianbao Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 12 p. 3115 - 3120

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被引用次数: 36

摘要

The 1, 4-benzodiazepine-2, 5-dione is a suitable template to disrupt the interaction between p53 and Hdm2. The development of an enantioselective synthesis disclosed the stereochemistry of the active enantiomer. An in vitro p53 peptide displacement assay identified active compounds. These activities were confirmed in several cell-based assays including induction of the p53 regulated gene (PIG-3) and caspase activity.