| Literature DB >> 16630722 |
Juan Jose Marugan1, Kristi Leonard, Pierre Raboisson, Joan M Gushue, Raul Calvo, Holly K Koblish, Jennifer Lattanze, Shuyuan Zhao, Maxwell D Cummings, Mark R Player, Carsten Schubert, Anna C Maroney, Tianbao Lu.
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.Entities:
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Year: 2006 PMID： 16630722 DOI： 10.1016/j.bmcl.2006.03.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823