Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists |
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| Authors: | 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 |
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| Affiliation: | Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 665 Stockton Drive, Exton, PA 19341, USA. jmaruga@prdus.jnj.com |
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| Abstract: | 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. |
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