Literature DB >> 24268795

Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.

Carlos J A Ribeiro1, Joana D Amaral1, Cecília M P Rodrigues1, Rui Moreira1, Maria M M Santos2.   

Abstract

Restoring p53 levels through disruption of p53-MDM2 interaction has been proved to be a valuable approach in fighting cancer. We herein report the synthesis and evaluation of eighteen spiroisoxazoline oxindoles derivatives as p53-MDM2 interaction inhibitors. Seven compounds showed an antiproliferative profile superior to the p53-MDM2 interaction inhibitor nutlin-3, and induced cell death by apoptosis. Moreover, proof-of-concept was demonstrated by inhibition of the interaction between p53 and MDM2 in a live-cell bimolecular fluorescence complementation assay.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cancer; MDM2; Protein–protein interactions; Spiro compounds; p53

Mesh：

Substances：

Year:  2013        PMID： 24268795     DOI： 10.1016/j.bmc.2013.10.048

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  6 in total

1.  Synthesis and antiproliferative and apoptosis-inducing activity of novel 3-substituted-3-hydroxy-2-oxindole compounds.

Authors:  Mona Nazemi Moghaddam; Razieh Jalal; Zohreh Zeraatkar
Journal:  In Vitro Cell Dev Biol Anim       Date:  2017-11-09       Impact factor: 2.416

2.  Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery.

Authors:  Thomas A King; Hannah L Stewart; Kim T Mortensen; Andrew J P North; Hannah F Sore; David R Spring
Journal:  European J Org Chem       Date:  2019-07-29

3.  Preparation of spiro[indole-3,5'-isoxazoles] via Grignard conjugate addition/spirocyclization sequence.

Authors:  Alexander V Aksenov; Dmitrii A Aksenov; Nicolai A Aksenov; Anton A Skomorokhov; Elena V Aleksandrova; Michael Rubin
Journal:  RSC Adv       Date:  2021-01-06       Impact factor: 3.361

Review 4.  Chemical Variations on the p53 Reactivation Theme.

Authors:  Carlos J A Ribeiro; Cecília M P Rodrigues; Rui Moreira; Maria M M Santos
Journal:  Pharmaceuticals (Basel)       Date:  2016-05-13

Review 5.  Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview.

Authors:  Dimitris Matiadis; Marina Sagnou
Journal:  Int J Mol Sci       Date:  2020-07-31       Impact factor: 5.923

6.  Targeted Synthesis of Complex Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors.

Authors:  Andreas Gollner; Harald Weinstabl; Julian E Fuchs; Dorothea Rudolph; Geraldine Garavel; Karin S Hofbauer; Jale Karolyi-Oezguer; Gerhard Gmaschitz; Wolfgang Hela; Nina Kerres; Elisabeth Grondal; Patrick Werni; Juergen Ramharter; Joachim Broeker; Darryl B McConnell
Journal:  ChemMedChem       Date:  2018-12-11       Impact factor: 3.466
  6 in total

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