Literature DB >> 18614366

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

Richard Angell1, Nicola M Aston, Paul Bamborough, Jacky B Buckton, Stuart Cockerill, Suzanne J deBoeck, Chris D Edwards, Duncan S Holmes, Katherine L Jones, Dramane I Laine, Shila Patel, Penny A Smee, Kathryn J Smith, Don O Somers, Ann L Walker.   

Abstract

The biphenyl amides (BPAs) are a novel series of p38alpha MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode.

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Year:  2008        PMID： 18614366     DOI： 10.1016/j.bmcl.2008.06.048

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


  12 in total

1.  Virtual screening using a conformationally flexible target protein: models for ligand binding to p38α MAPK.

Authors:  Natalie B Vinh; Jamie S Simpson; Peter J Scammells; David K Chalmers
Journal:  J Comput Aided Mol Des       Date:  2012-04-20       Impact factor: 3.686

2.  Investigation of differences in the binding affinities of two analogous ligands for untagged and tagged p38 kinase using thermodynamic integration MD simulation.

Authors:  Ying-Chieh Sun; Wen-Chi Hsu; Chia-Jen Hsu; Chia-Ming Chang; Kai-Hsiang Cheng
Journal:  J Mol Model       Date:  2015-10-08       Impact factor: 1.810

3.  Palladium-Catalyzed Methylation of Aryl, Heteroaryl, and Vinyl Boronate Esters.

Authors:  Alexander M Haydl; John F Hartwig
Journal:  Org Lett       Date:  2019-02-14       Impact factor: 6.005

4.  Methyl effects on protein-ligand binding.

Authors:  Cheryl S Leung; Siegfried S F Leung; Julian Tirado-Rives; William L Jorgensen
Journal:  J Med Chem       Date:  2012-04-23       Impact factor: 7.446

5.  3D-QSAR and molecular docking analysis of biphenyl amide derivatives as p38α mitogen-activated protein kinase inhibitors.

Authors:  Pravin Sundarao Ambure; Rahul Prakashchand Gangwal; Abhay T Sangamwar
Journal:  Mol Divers       Date:  2012-01-07       Impact factor: 2.943

6.  Estimation of relative free energies of binding using pre-computed ensembles based on the single-step free energy perturbation and the site-identification by Ligand competitive saturation approaches.

Authors:  E Prabhu Raman; Sirish Kaushik Lakkaraju; Rajiah Aldrin Denny; Alexander D MacKerell
Journal:  J Comput Chem       Date:  2016-10-26       Impact factor: 3.376

7.  Rosiglitazone inhibits TGF-β 1 induced activation of human Tenon fibroblasts via p38 signal pathway.

Authors:  Yong-Heng Luo; Ping-Bo Ouyang; Jiao Tian; Xiao-Jian Guo; Xuan-Chu Duan
Journal:  PLoS One       Date:  2014-08-21       Impact factor: 3.240

8.  Modifications of the Triaminoaryl Metabophore of Flupirtine and Retigabine Aimed at Avoiding Quinone Diimine Formation.

Authors:  Konrad W Wurm; Frieda-Marie Bartz; Lukas Schulig; Anja Bodtke; Patrick J Bednarski; Andreas Link
Journal:  ACS Omega       Date:  2022-02-25

9.  Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Authors:  Patricia Dranchak; Ryan MacArthur; Rajarshi Guha; William J Zuercher; David H Drewry; Douglas S Auld; James Inglese
Journal:  PLoS One       Date:  2013-03-07       Impact factor: 3.240

10.  Rational Design of Benzylidenehydrazinyl-Substituted Thiazole Derivatives as Potent Inhibitors of Human Dihydroorotate Dehydrogenase with in Vivo Anti-arthritic Activity.

Authors:  Shiliang Li; Guoqin Luan; Xiaoli Ren; Wenlin Song; Liuxin Xu; Minghao Xu; Junsheng Zhu; Dong Dong; Yanyan Diao; Xiaofeng Liu; Lili Zhu; Rui Wang; Zhenjiang Zhao; Yufang Xu; Honglin Li
Journal:  Sci Rep       Date:  2015-10-07       Impact factor: 4.379
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