Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 3, 2010, Pages 1293-1297

  Velcicky, Juraj ^a   Feifel, Roland ^a   Hawtin, Stuart ^a   Heng, Richard ^a   Huppertz, Christine ^a   Koch, Guido ^a   Kroemer, Markus ^a   Moebitz, Henrik ^a   Revesz, Laszlo ^a   Scheufler, Clemens ^a   Schlapbach, Achim ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

3 Aminopyrazole; Induced fit; MK2; Scaffold hopping; TNF inhibition; X ray

Indexed keywords

HEAT SHOCK PROTEIN 27; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE ACTIVATED PROTEIN KINASE 2; MITOGEN ACTIVATED PROTEIN KINASE ACTIVATED PROTEIN KINASE 2 INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE P38; PHOSPHOTRANSFERASE INHIBITOR; PYRAZOLE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA; TUMOR NECROSIS FACTOR ALPHA ANTIBODY; UNCLASSIFIED DRUG; 3-AMINOPYRAZOLE; MAP-KINASE-ACTIVATED KINASE 2; PROTEIN SERINE THREONINE KINASE; SIGNAL PEPTIDE;

ANIMAL EXPERIMENT; ARTICLE; CYTOKINE RELEASE; DRUG DOSE COMPARISON; DRUG PROTEIN BINDING; DRUG STRUCTURE; ENZYME INHIBITION; FEMALE; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; IC 50; MOUSE; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PHARMACOPHORE; PROTEIN PHOSPHORYLATION; ANTAGONISTS AND INHIBITORS; CELL CULTURE; CHEMISTRY; COMPARATIVE STUDY; DRUG DEVELOPMENT; METABOLISM; PROCEDURES; PROTEIN CONFORMATION; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

CELL LINE, TUMOR; CELLS, CULTURED; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; PROTEIN CONFORMATION; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES;

EID: 74049123532     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.138     Document Type: Article

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