Discovery and optimization of 1,3,5-trisubstituted pyrazolines as potent and highly selective allosteric inhibitors of protein kinase C-χ

Journal of Medicinal Chemistry

Volumn 57, Issue 15, 2014, Pages 6513-6530

  Abdel Halim, Mohammad ^a,b   Diesel, Britta ^a   Kiemer, Alexandra K ^a   Abadi, Ashraf H ^b   Hartmann, Rolf W ^a   Engel, Matthias ^a  

^a SAARLAND UNIVERSITY   (Germany)

^b German University in Cairo   (Egypt)

Author keywords

[No Author keywords available]

Indexed keywords

1 (3 CHLOROPHENYL) 5 (3 FLUORO 4 METHOXYPHENYL) 3 (2 METHOXYPHENYL) 4 METHYL 4,5 DIHYDRO 1H PYRAZOLE; 1 [4 (TERT BUTOXY)PHENYL] 4,4 DIMETHYLPENT 1 EN 3 ONE; 4 [1 (3 CHLOROPHENYL) 5 (3 FLUORO 4 HYDROXYPHENYL) 4,5 DIHYDRO 1H PYRAZOL 3 YL]BENZENE 1,3 DIOL; 4 [3 (TERT BUTYL) 1 (3,4 DIFLUOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 5 YL]PHENOL; 4 [3 (TERT BUTYL) 1 (4 CHLOROPHENYL) 4,5 DIHYDRO 1H PYRAZOL 5 YL]PHENOL; PHENAZONE DERIVATIVE; PROTEIN KINASE C INHIBITOR; UNCLASSIFIED DRUG; ANTIINFLAMMATORY AGENT; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; NITRIC OXIDE; PROTEIN KINASE C; PROTEIN KINASE C BETA; PROTEIN KINASE C ZETA; PYRAZOLE DERIVATIVE; RECOMBINANT PROTEIN;

ARTICLE; ASSAY; BINDING SITE; CATALYSIS; CONTROLLED STUDY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; EMBRYO; ENZYME ACTIVE SITE; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; MOLECULAR INTERACTION; REPORTER GENE; STRUCTURE ACTIVITY RELATION; WESTERN BLOTTING; ALLOSTERISM; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOSYNTHESIS; CHEMISTRY; DRUG EFFECTS; ENZYME STABILITY; GENETICS; HEK293 CELL LINE; MACROPHAGE; METABOLISM; MOLECULAR DOCKING; MOUSE; MUTATION; PHOSPHORYLATION; SIGNAL TRANSDUCTION; SYNTHESIS; U937 CELL LINE;

ALLOSTERIC REGULATION; ANIMALS; ANTI-INFLAMMATORY AGENTS; CATALYTIC DOMAIN; ENZYME STABILITY; HEK293 CELLS; HUMANS; MACROPHAGES; MICE; MOLECULAR DOCKING SIMULATION; MUTATION; NF-KAPPA B; NITRIC OXIDE; PHOSPHORYLATION; PROTEIN KINASE C; PROTEIN KINASE C BETA; PYRAZOLES; RECOMBINANT PROTEINS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; U937 CELLS;

EID: 84906092136     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500521n     Document Type: Article

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