| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377452 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Juan Jose Marugan, 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,