Literature DB >> 12039561

Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.

Jacques Dumas1, Holia Hatoum-Mokdad, Robert N Sibley, Roger A Smith, William J Scott, Uday Khire, Wendy Lee, Jill Wood, Donald Wolanin, Jeffrey Cooley, Donald Bankston, Aniko M Redman, Robert Schoenleber, Yolanda Caringal, David Gunn, Romulo Romero, Martin Osterhout, Holger Paulsen, Timothy J Housley, Scott M Wilhelm, John Pirro, Du-Shieng Chien, Gerald E Ranges, Alka Shrikhande, Andrew Muzsi, Elizabeth Bortolon, Jean Wakefield, Cynthia Gianpaolo Ostravage, Ajay Bhargava, Thuy Chau.   

Abstract

Inhibitors of the MAP kinase p38 provide a novel approach for the treatment of osteoporosis, inflammatory disorders, and cancer. We have identified N-(3-tert-butyl-1-methyl-5-pyrazolyl)-N'-(4-(4-pyridinylmethyl)phenyl)urea as a potent and selective p38 kinase inhibitor in biochemical and cellular assays. This compound is orally active in two acute models of cytokine release (TNF-induced IL-6 and LPS-induced TNF) and a chronic model of arthritis (20-day murine collagen-induced arthritis).

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Year:  2002        PMID: 12039561     DOI: 10.1016/s0960-894x(02)00238-x

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


  4 in total

1.  Strategies to design pyrazolyl urea derivatives for p38 kinase inhibition: a molecular modeling study.

Authors:  Ravindra G Kulkarni; Palukuri Srivani; Garlapati Achaiah; G Narahari Sastry
Journal:  J Comput Aided Mol Des       Date:  2007-01-04       Impact factor: 3.686

Review 2.  Novel host response therapeutic approaches to treat periodontal diseases.

Authors:  Keith L Kirkwood; Joni A Cirelli; Jill E Rogers; William V Giannobile
Journal:  Periodontol 2000       Date:  2007       Impact factor: 7.589

Review 3.  The p38 mitogen-activated protein kinase signaling cascade in CD4 T cells.

Authors:  Francis Dodeller; Hendrik Schulze-Koops
Journal:  Arthritis Res Ther       Date:  2006-02-17       Impact factor: 5.156

Review 4.  Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry.

Authors:  Chiara Brullo; Federica Rapetti; Olga Bruno
Journal:  Molecules       Date:  2020-07-29       Impact factor: 4.411

  4 in total

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