Literature DB >> 10999468

1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.

J Dumas1, H Hatoum-Mokdad, R Sibley, B Riedl, W J Scott, M K Monahan, T B Lowinger, C Brennan, R Natero, T Turner, J S Johnson, R Schoenleber, A Bhargava, S M Wilhelm, T J Housley, G E Ranges, A Shrikhande.   

Abstract

Inhibitors of the MAP kinase p38 are potentially useful for the treatment of arthritis and osteoporosis. Several 2,3-dichlorophenyl ureas were identified as small-molecule inhibitors of p38 by a combinatorial chemistry effort. Optimization for cellular potency led to the discovery of a new class of potent and selective p38 kinase inhibitors, exemplified by the 1-phenyl-5-pyrazolyl urea 7 (IC50 = 13 nM).

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Year:  2000        PMID: 10999468     DOI: 10.1016/s0960-894x(00)00272-9

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


  8 in total

1.  Modified AutoDock for accurate docking of protein kinase inhibitors.

Authors:  Oleksandr V Buzko; Anthony C Bishop; Kevan M Shokat
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2.  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 3.  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

4.  A new screening assay for allosteric inhibitors of cSrc.

Authors:  Jeffrey R Simard; Sabine Klüter; Christian Grütter; Matthäus Getlik; Matthias Rabiller; Haridas B Rode; Daniel Rauh
Journal:  Nat Chem Biol       Date:  2009-04-26       Impact factor: 15.040

5.  Sequence determinants of a specific inactive protein kinase conformation.

Authors:  Sanjay B Hari; Ethan A Merritt; Dustin J Maly
Journal:  Chem Biol       Date:  2013-06-20

6.  Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src.

Authors:  Sanjay B Hari; B Gayani K Perera; Pratistha Ranjitkar; Markus A Seeliger; Dustin J Maly
Journal:  ACS Chem Biol       Date:  2013-10-29       Impact factor: 5.100

7.  Crystal structure of (Z)-ethyl 3-[2-(5-methyl-7-nitro-1H-indole-2-carbon-yl)hydrazinyl-idene]butano-ate.

Authors:  Amal Errossafi; Abdellatif El Kihel; Salaheddine Guesmi; Mohamed Saadi; Lahcen El Ammari
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-08-22

Review 8.  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

  8 in total

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