Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38α mitogen-activated protein kinase

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 5, 2010, Pages 1680-1684

  Wurz, Ryan P ^a   Pettus, Liping H ^a   Henkle, Bradley ^a   Sherman, Lisa ^a   Plant, Matthew ^a   Miner, Kent ^a   McBride, Helen J ^a   Wong, Lu Min ^a   Saris, Christiaan J M ^a   Lee, Matthew R ^a   Chmait, Samer ^a   Mohr, Christopher ^a   Hsieh, Faye ^a   Tasker, Andrew S ^a  

^a AMGEN INC   (United States)

Author keywords

MAP kinase; p38; Pyrazolopyridazine; TNF

Indexed keywords

ANTIINFLAMMATORY AGENT; INTERLEUKIN 8; LIPOPOLYSACCHARIDE; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; PYRAZOLE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BLOOD; CRYSTAL STRUCTURE; CYTOKINE PRODUCTION; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG SCREENING; DRUG STRUCTURE; IC 50; LEWIS RAT; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; BENZAMIDES; BINDING SITES; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; HUMANS; INTERLEUKIN-8; LIPOPOLYSACCHARIDES; MALE; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN KINASE INHIBITORS; PYRAZOLES; PYRIDAZINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR NECROSIS FACTOR-ALPHA;

RATTUS;

EID: 76649099501     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.059     Document Type: Article

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