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Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors

Journal Article · · Bioorganic and Medicinal Chemistry
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Not Available
Sponsoring Organization:
USDOE
OSTI ID:
1548864
Journal Information:
Bioorganic and Medicinal Chemistry, Journal Name: Bioorganic and Medicinal Chemistry Journal Issue: 3 Vol. 26; ISSN 0968-0896
Publisher:
ElsevierCopyright Statement
Country of Publication:
United Kingdom
Language:
English

References (25)

Activation, differential localization, and regulation of the stress-activated protein kinases, extracellular signal-regulated kinase, c-Jun N-terminal kinase, and p38 mitogen-activated protein kinase, in synovial tissue and cells in rheumatoid arthritis journal November 2000
Discovery and Characterization of Atropisomer PH-797804, a p38 MAP Kinase Inhibitor, as a Clinical Drug Candidate journal December 2011
The role of p38 mitogen-activated protein kinase in IL-6 and IL-8 production from the TNF-α- or IL-1β-stimulated rheumatoid synovial fibroblasts journal December 1999
Stress-activated Protein Kinases: Activation, Regulation and Function journal September 1997
High throughput P450 inhibition screens in early drug discovery journal November 2005
A novel p38 mitogen activated protein kinase (MAPK) specific inhibitor suppresses respiratory syncytial virus and influenza A virus replication by inhibiting virus-induced p38 MAPK activation journal August 2016
Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept journal August 2014
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase journal April 2010
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase journal July 2011
Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors journal September 2015
Emerging trends in the therapy of COPD: novel anti-inflammatory agents in clinical development journal June 2007
Emerging therapeutic strategies in COPD journal March 2015
MAP Kinases journal August 2001
Pyrazole Urea-Based Inhibitors of p38 MAP Kinase:  From Lead Compound to Clinical Candidate journal July 2002
Novel Inhibitor of p38 MAP Kinase as an Anti-TNF-α Drug:  Discovery of N -[4-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a Potent and Orally Active Anti-Rheumatoid Arthritis Agent journal September 2005
Identification, Synthesis, and Biological Evaluation of 6-[(6 R )-2-(4-Fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5- a ]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2 H )-one (AS1940477), a Potent p38 MAP Kinase Inhibitor journal August 2012
Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1 H -pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia † † Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1). journal August 2009
Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders journal December 2009
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis journal December 1994
p38 MAP kinases: key signalling molecules as therapeutic targets for inflammatory diseases journal September 2003
Pro-inflammatory Cytokines and Environmental Stress Cause p38 Mitogen-activated Protein Kinase Activation by Dual Phosphorylation on Tyrosine and Threonine journal March 1995
X-ray structure of p38α bound to TAK-715: comparison with three classic inhibitors journal July 2012
Synthesis and Biological Activities of 4-Phenyl-5-pyridyl-1,3-thiazole Derivatives as p38 MAP Kinase Inhibitors journal January 2005
MAP Kinase p38Inhibitors: Clinical Results and an Intimate Look at Their Interactions with p38α Protein journal December 2005
P38 MAP Kinase Inhibitors: Evolution of Imidazole-Based and Pyrido- Pyrimidin-2-One Lead Classes journal September 2005

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