Literature DB >> 11354358

Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles.

J C Boehm1, M J Bower, T F Gallagher, S Kassis, S R Johnson, J L Adams.   

Abstract

As a continuation of our work with 1,4,5 substituted imidazole inhibitors of p38alpha, we report a series of 1-(4-piperidinyl)-4-(4-fluorophenyl)-5-(2-phenoxy-4-pyrimidinyl) imidazoles related to 7. The compounds have IC50's for inhibition of p38alpha ranging from 6.0 to 650nM. Statistical analysis of the p38beta inhibitor potencies shows a correlation of IC50's with the electron donating strength of low molecular weight substituents.

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Year:  2001        PMID: 11354358     DOI: 10.1016/s0960-894x(01)00163-9

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


  11 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.  MAP kinases: differential activation following in vivo and ex vivo irradiation.

Authors:  Anirban Kumar Mitra; Rakesh Kumar Singh; Malini Krishna
Journal:  Mol Cell Biochem       Date:  2006-11-29       Impact factor: 3.396

3.  Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors.

Authors:  Angela S Carlson; Huarui Cui; Anand Divakaran; Jorden A Johnson; Ryan M Brunner; William C K Pomerantz; Joseph J Topczewski
Journal:  ACS Med Chem Lett       Date:  2019-08-02       Impact factor: 4.345

4.  Construction of 4D-QSAR models for use in the design of novel p38-MAPK inhibitors.

Authors:  Nelilma Correia Romeiro; Magaly Girão Albuquerque; Ricardo Bicca de Alencastro; Malini Ravi; Anton J Hopfinger
Journal:  J Comput Aided Mol Des       Date:  2005-06       Impact factor: 3.686

5.  Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules.

Authors:  Andrew K Urick; Laura M L Hawk; Melissa K Cassel; Neeraj K Mishra; Shuai Liu; Neeta Adhikari; Wei Zhang; Camila O dos Santos; Jennifer L Hall; William C K Pomerantz
Journal:  ACS Chem Biol       Date:  2015-07-28       Impact factor: 5.100

6.  Free-energy force-field three-dimensional quantitative structure-activity relationship analysis of a set of p38-mitogen activated protein kinase inhibitors.

Authors:  Nelilma Correia Romeiro; Magaly Girão Albuquerque; Ricardo Bicca de Alencastro; Malini Ravi; Anton J Hopfinger
Journal:  J Mol Model       Date:  2006-03-16       Impact factor: 1.810

7.  Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.

Authors:  Anand Divakaran; Siva K Talluri; Alex M Ayoub; Neeraj K Mishra; Huarui Cui; John C Widen; Norbert Berndt; Jin-Yi Zhu; Angela S Carlson; Joseph J Topczewski; Ernst K Schonbrunn; Daniel A Harki; William C K Pomerantz
Journal:  J Med Chem       Date:  2018-10-16       Impact factor: 7.446

8.  Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases.

Authors:  Martina Hrast; Kaja Rožman; Iza Ogris; Veronika Škedelj; Delphine Patin; Matej Sova; Hélène Barreteau; Stanislav Gobec; Simona Golič Grdadolnik; Anamarija Zega
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

9.  The inflammatory kinase MAP4K4 promotes reactivation of Kaposi's sarcoma herpesvirus and enhances the invasiveness of infected endothelial cells.

Authors:  Darya A Haas; Kiran Bala; Guntram Büsche; Magdalena Weidner-Glunde; Susann Santag; Semra Kati; Silvia Gramolelli; Modester Damas; Oliver Dittrich-Breiholz; Michael Kracht; Jessica Rückert; Zoltan Varga; György Keri; Thomas F Schulz
Journal:  PLoS Pathog       Date:  2013-11-07       Impact factor: 6.823

10.  GATA-3 regulates the self-renewal of long-term hematopoietic stem cells.

Authors:  Catherine Frelin; Robert Herrington; Salima Janmohamed; Mary Barbara; Gary Tran; Christopher J Paige; Patricia Benveniste; Juan-Carlos Zuñiga-Pflücker; Abdallah Souabni; Meinrad Busslinger; Norman N Iscove
Journal:  Nat Immunol       Date:  2013-08-25       Impact factor: 25.606

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