Title of article
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
3115
To page
3120
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.
Keywords
Hdm2 , Protein–protein interaction , p53
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796937
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