Author/Authors :
Juan Jose Marugan، نويسنده , , Kristi Leonard، نويسنده , , Pierre Raboisson، نويسنده , , Joan M. Gushue، نويسنده , , Raul Calvo، نويسنده , , Holly K. Koblish، نويسنده , , Jennifer Lattanze، نويسنده , , Shuyuan Zhao، نويسنده , , Maxwell D. Cummings، نويسنده , , Mark R. Player، نويسنده , , Paul B. Sigler and Carsten Schubert، نويسنده , , Anna C. Maroney، نويسنده , , Tianbao Lu، نويسنده ,
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.
