Literature DB >> 16600594

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.

Daniel J Parks1, Louis V LaFrance, Raul R Calvo, Karen L Milkiewicz, Juan José Marugán, Pierre Raboisson, Carsten Schubert, Holly K Koblish, Shuyuan Zhao, Carol F Franks, Jennifer Lattanze, Theodore E Carver, Maxwell D Cummings, Diane Maguire, Bruce L Grasberger, Anna C Maroney, Tianbao Lu.   

Abstract

Guided by structure-based drug design, modification of the 1,4-benzodiazepin-2,5-dione lead compound 1 resulted in the discovery of 19, a potent and orally bioavailable antagonist of the HDM2-p53 protein-protein interaction (FP IC50 = 0.7 microM, F approximately 100%).

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Year:  2006        PMID： 16600594     DOI： 10.1016/j.bmcl.2006.03.055

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  24 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

2.  Beta-peptides with improved affinity for hDM2 and hDMX.

Authors:  Elizabeth A Harker; Douglas S Daniels; Danielle A Guarracino; Alanna Schepartz
Journal:  Bioorg Med Chem       Date:  2009-01-23       Impact factor: 3.641

3.  Ligand binding mode prediction by docking: mdm2/mdmx inhibitors as a case study.

Authors:  Nagakumar Bharatham; Kavitha Bharatham; Anang A Shelat; Donald Bashford
Journal:  J Chem Inf Model       Date:  2014-01-21       Impact factor: 4.956

Review 4.  The structure-based design of Mdm2/Mdmx-p53 inhibitors gets serious.

Authors:  Grzegorz M Popowicz; Alexander Dömling; Tad A Holak
Journal:  Angew Chem Int Ed Engl       Date:  2011-02-21       Impact factor: 15.336

5.  Simulation of MDM2 N-terminal domain conformational lability in the presence of imidazoline based inhibitors of MDM2-p53 protein-protein interaction.

Authors:  Maxim Gureev; Daria Novikova; Tatyana Grigoreva; Svetlana Vorona; Alexander Garabadzhiu; Vyacheslav Tribulovich
Journal:  J Comput Aided Mol Des       Date:  2019-11-28       Impact factor: 3.686

6.  1,4-Thienodiazepine-2,5-diones via MCR (II): scaffold hopping by Gewald and Ugi-deprotection-cyclization strategy.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Chem Biol Drug Des       Date:  2010-06-09       Impact factor: 2.817

7.  Structural conservation in band 4.1, ezrin, radixin, moesin (FERM) domains as a guide to identify inhibitors of the proline-rich tyrosine kinase 2.

Authors:  Nathalie Meurice; Lei Wang; Christopher A Lipinski; Zhongbo Yang; Christopher Hulme; Joseph C Loftus
Journal:  J Med Chem       Date:  2010-01-28       Impact factor: 7.446

Review 8.  Targeting Mdm2 and Mdmx in cancer therapy: better living through medicinal chemistry?

Authors:  Mark Wade; Geoffrey M Wahl
Journal:  Mol Cancer Res       Date:  2009-01       Impact factor: 5.852

9.  The p53-MDM2/MDMX axis - A chemotype perspective.

Authors:  Kareem Khoury; Grzegorz M Popowicz; Tad A Holak; Alexander Dömling
Journal:  Medchemcomm       Date:  2011       Impact factor: 3.597

Review 10.  Awakening guardian angels: drugging the p53 pathway.

Authors:  Christopher J Brown; Sonia Lain; Chandra S Verma; Alan R Fersht; David P Lane
Journal:  Nat Rev Cancer       Date:  2009-12       Impact factor: 60.716
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