Literature DB >> 16647257

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity.

Kristi Leonard1, Juan Jose Marugan, Pierre Raboisson, Raul Calvo, Joan M Gushue, Holly K Koblish, Jennifer Lattanze, Shuyuan Zhao, Maxwell D Cummings, Mark R Player, Anna C Maroney, Tianbao Lu.   

Abstract

The disruption of the p53-Hdm2 protein-protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.

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Year:  2006        PMID： 16647257     DOI： 10.1016/j.bmcl.2006.04.009

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


  14 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.  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

3.  Synthesis of phantasmidine.

Authors:  Quan Zhou; Barry B Snider
Journal:  Org Lett       Date:  2010-12-22       Impact factor: 6.005

4.  1,4-Thienodiazepine-2,5-diones via MCR (I): synthesis, virtual space and p53-Mdm2 activity.

Authors:  Yijun Huang; Siglinde Wolf; Michal Bista; Lidio Meireles; Carlos Camacho; Tad A Holak; Alexander Dömling
Journal:  Chem Biol Drug Des       Date:  2010-05-18       Impact factor: 2.817

5.  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 6.  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

Review 7.  Privileged diazepine compounds and their emergence as bromodomain inhibitors.

Authors:  Steven G Smith; Roberto Sanchez; Ming-Ming Zhou
Journal:  Chem Biol       Date:  2014-04-17

Review 8.  Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy.

Authors:  Sanjeev Shangary; Shaomeng Wang
Journal:  Annu Rev Pharmacol Toxicol       Date:  2009       Impact factor: 13.820

9.  Microwave-assisted fluorous synthesis of a 1,4-benzodiazepine-2,5-dione library.

Authors:  Aifeng Liu; Hongyu Zhou; Gaoxing Su; Wei Zhang; Bing Yan
Journal:  J Comb Chem       Date:  2009 Nov-Dec

10.  Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions.

Authors:  Alex Shaginian; Landon R Whitby; Sukwon Hong; Inkyu Hwang; Bilal Farooqi; Mark Searcey; Jiandong Chen; Peter K Vogt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2009-04-22       Impact factor: 15.419
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