Literature DB >> 20079636

Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.

Yann Lamotte1, Paul Martres, Nicolas Faucher, Alain Laroze, Didier Grillot, Nicolas Ancellin, Yannick Saintillan, Véronique Beneton, Robert T Gampe.   

Abstract

Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPARgamma ligand binding domain is described. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20079636     DOI： 10.1016/j.bmcl.2009.12.107

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


  10 in total

1.  Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.

Authors:  Alice Asteian; Anne-Laure Blayo; Yuanjun He; Marcel Koenig; Youseung Shin; Dana S Kuruvilla; Cesar A Corzo; Michael D Cameron; Li Lin; Claudia Ruiz; Susan Khan; Naresh Kumar; Scott Busby; David P Marciano; Ruben D Garcia-Ordonez; Patrick R Griffin; Theodore M Kamenecka
Journal:  ACS Med Chem Lett       Date:  2015-08-04       Impact factor: 4.345

2.  Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.

Authors:  Venkateswararao Eeda; Dan Wu; Hui-Ying Lim; Weidong Wang
Journal:  Bioorg Med Chem Lett       Date:  2019-09-03       Impact factor: 2.823

3.  Structural insights for the design of new PPARgamma partial agonists with high binding affinity and low transactivation activity.

Authors:  Laura Guasch; Esther Sala; Cristina Valls; Mayte Blay; Miquel Mulero; Lluís Arola; Gerard Pujadas; Santiago Garcia-Vallvé
Journal:  J Comput Aided Mol Des       Date:  2011-06-21       Impact factor: 3.686

4.  SR2067 Reveals a Unique Kinetic and Structural Signature for PPARγ Partial Agonism.

Authors:  Laura M van Marrewijk; Steven W Polyak; Marcel Hijnen; Dana Kuruvilla; Mi Ra Chang; Youseung Shin; Theodore M Kamenecka; Patrick R Griffin; John B Bruning
Journal:  ACS Chem Biol       Date:  2015-12-03       Impact factor: 5.100

5.  Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation.

Authors:  Jang Hyun Choi; Alexander S Banks; Theodore M Kamenecka; Scott A Busby; Michael J Chalmers; Naresh Kumar; Dana S Kuruvilla; Youseung Shin; Yuanjun He; John B Bruning; David P Marciano; Michael D Cameron; Dina Laznik; Michael J Jurczak; Stephan C Schürer; Dušica Vidović; Gerald I Shulman; Bruce M Spiegelman; Patrick R Griffin
Journal:  Nature       Date:  2011-09-04       Impact factor: 49.962

6.  Identification of a novel selective PPARγ ligand with a unique binding mode and improved therapeutic profile in vitro.

Authors:  Wei Yi; Jingjing Shi; Guanguan Zhao; X Edward Zhou; Kelly Suino-Powell; Karsten Melcher; H Eric Xu
Journal:  Sci Rep       Date:  2017-01-27       Impact factor: 4.379

7.  Dual vicinal functionalisation of heterocycles via an interrupted Pummerer coupling/[3,3]-sigmatropic rearrangement cascade.

Authors:  Mindaugas Šiaučiulis; Selma Sapmaz; Alexander P Pulis; David J Procter
Journal:  Chem Sci       Date:  2017-11-17       Impact factor: 9.825

Review 8.  New Insights into the PPAR γ Agonists for the Treatment of Diabetic Nephropathy.

Authors:  Zhanjun Jia; Ying Sun; Guangrui Yang; Aihua Zhang; Songming Huang; Kristina Marie Heiney; Yue Zhang
Journal:  PPAR Res       Date:  2014-01-29       Impact factor: 4.964

9.  An alternate binding site for PPARγ ligands.

Authors:  Travis S Hughes; Pankaj Kumar Giri; Ian Mitchelle S de Vera; David P Marciano; Dana S Kuruvilla; Youseung Shin; Anne-Laure Blayo; Theodore M Kamenecka; Thomas P Burris; Patrick R Griffin; Douglas J Kojetin
Journal:  Nat Commun       Date:  2014-04-07       Impact factor: 14.919

10.  Synthesis and Characterization of Telmisartan-Derived Cell Death Modulators to Circumvent Imatinib Resistance in Chronic Myeloid Leukemia.

Authors:  Anna M Schoepf; Stefan Salcher; Verena Hohn; Florina Veider; Petra Obexer; Ronald Gust
Journal:  ChemMedChem       Date:  2020-05-06       Impact factor: 3.466
  10 in total

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