Structure-based design, synthesis and biological evaluation of N-pyrazole, N′-thiazole urea inhibitors of MAP kinase p38α

European Journal of Medicinal Chemistry

Volumn 48, Issue , 2012, Pages 1-15

  Getlik, Matthäus ^a   Grütter, Christian ^a,b   Simard, Jeffrey R ^a   Nguyen, Hoang D ^a   Robubi, Armin ^a   Aust, Beate ^a   Van Otterlo, Willem A L ^c,d   Rauh, Daniel ^a,b  

^a CHEMICAL GENOMICS CENTRE OF THE MAX PLANCK SOCIETY   (Germany)

^b TU DORTMUND UNIVERSITY   (Germany)

^c UNIVERSITY OF THE WITWATERSRAND   (South Africa)

^d STELLENBOSCH UNIVERSITY   (South Africa)

Author keywords

DFG out; Kinase inhibitors; p38 MAPK

Indexed keywords

[3 [5 [[[[4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL]AMINO]CARBONYL]AMINO] 3 CYCLOPENTYL 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; [3 [5 [[[[4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL]AMINO]CARBONYL]AMINO] 3 CYCLOPROPYL 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; [3 [5 [[[[4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL]AMINO]CARBONYL]AMINO] 3 TERT BUTYL 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; [4 [3 TERT BUTYL 5 [[(1,3 THIAZOL 2 YLAMINO)CARBONYL]AMINO] 1H PYRAZOL 1 YL]PHENYL]ACETATE; [4 [3 TERT BUTYL 5 [[(1,3 THIAZOL 2 YLAMINO)CARBONYL]AMINO] 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; [4 [5 [[[[4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL]AMINO]CARBONYL]AMINO] 3 CYCLOPENTYL 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; [4 [5 [[[[4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL]AMINO]CARBONYL]AMINO] 3 TERT BUTYL 1H PYRAZOL 1 YL]PHENYL]ACETIC ACID; ETHYL [4 [3 TERT BUTYL 5 [[(1,3 THIAZOL 2 YLAMINO)CARBONYL]AMINO] 1H PYRAZOL 1 YL]PHENYL]ACETATE; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; N [3 TERT BUTYL 1 (4 METHYLPHENYL) 1H PYRAZOL 5 YL] N' (1,3 THIAZOL 2 YL)UREA; N [3 TERT BUTYL 1 (4 METHYLPHENYL) 1H PYRAZOL 5 YL] N' [4 [2 (4 PYRIDINYLMETHOXY)ETHYL] 1,3 THIAZOL 2 YL]UREA; N [3 TERT BUTYL 1 (4 METHYLPHENYL) 1H PYRAZOL 5 YL] N' [4 [2 [(4 FLUOROBENZYL)OXY]ETHYL] 1,3 THIAZOL 2 YL]UREA; N [4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL] 3 FLUORO 5 (4 MORPHOLINYL)BENZAMIDE; N [4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL] N' [3 TERT BUTYL 1 (4 METHYLPHENYL) 1H PYRAZOL 5 YL]UREA; N [4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YL] N' [4 CHLORO 3 (TRIFLUOROMETHYL)PHENYL]UREA; PYRAZOLE DERIVATIVE; TERT BUTYL 4 (2 HYDROXYETHYL) 1,3 THIAZOL 2 YLCARBAMATE; TERT BUTYL 4 [2 (4 PYRIDINYLMETHOXY)ETHYL] 1,3 THIAZOL 2 YLCARBAMATE; TERT BUTYL 4 [2 (BENZYLOXY)ETHYL] 1,3 THIAZOL 2 YLCARBAMATE; TERT BUTYL 4 [2 [(4 FLUOROBENZYL)OXY]ETHYL] 1,3 THIAZOL 2 YLCARBAMATE; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ARTICLE; BIOLOGICAL ACTIVITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME PHOSPHORYLATION; FEMALE; HELA CELL; HUMAN; HUMAN CELL; PHARMACOLOGICAL BLOCKING;

HUMANS; INHIBITORY CONCENTRATION 50; MAGNETIC RESONANCE SPECTROSCOPY; MITOGEN-ACTIVATED PROTEIN KINASE 14; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PYRAZOLES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; UREA; X-RAY DIFFRACTION;

EID: 84855999356     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2011.11.019     Document Type: Article

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