Optimization of α-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 16, 2010, Pages 4819-4824

  Montalban, Antonio Garrido ^a   Boman, Erik ^a   Chang, Chau Dung ^a   Ceide, Susana Conde ^a   Dahl, Russell ^a   Dalesandro, David ^a   Delaet, Nancy G J ^a   Erb, Eric ^a   Ernst, Justin T ^a   Gibbs, Andrew ^a   Kahl, Jeffrey ^a   Kessler, Linda ^a   Kucharski, Jeff ^a   Lum, Christopher ^a   Lundström, Jan ^a   Miller, Stephen ^a   Nakanishi, Hiroshi ^a   Roberts, Edward ^a   Saiah, Eddine ^a   Sullivan, Robert ^a   Urban, Jan ^a   Wang, Zhijun ^a   Larson, Christopher J ^a   more..

^a Kemia Inc   (United States)

Author keywords

Antiinflammatory; Cytokines; Drug like; Ketoamides; p38 MAP kinase; SAR

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; ADENOSINE TRIPHOSPHATE; ALPHA KETOAMIDE; AMIDE; DORAMAPIMOD; MITOGEN ACTIVATED PROTEIN KINASE P38; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; NONSTEROID ANTIINFLAMMATORY AGENT; PROTEIN BINDING; PROTEIN KINASE INHIBITOR;

ALLOSTERISM; ANIMAL EXPERIMENT; ANTIINFLAMMATORY ACTIVITY; ARTICLE; BINDING SITE; CHEMICAL MODIFICATION; CONTACT ALLERGY; CYTOKINE PRODUCTION; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG SYNTHESIS; DRUG TARGETING; ENZYME INHIBITION; HUMAN; HUMAN CELL; HYPERSENSITIVITY; IC 50; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; MONOCYTE; NONHUMAN; PHARMACOPHORE; RAT; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; CHEMISTRY; COMPUTER SIMULATION; METABOLISM; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ADMINISTRATION, ORAL; ALLOSTERIC SITE; AMIDES; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BINDING SITES; CELL LINE; COMPUTER SIMULATION; HUMANS; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77955420030     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.102     Document Type: Article

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