Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-jun n-terminal kinase

Journal of Medicinal Chemistry

Volumn 52, Issue 7, 2009, Pages 1943-1952

  De, Surya K ^a   Stebbins, John L ^a   Chen, Li Hsing ^a   Riel Mehan, Megan ^a   Machleidt, Thomas ^b   Dahl, Russell ^a   Yuan, Hongbin ^a   Emdadi, Aras ^a   Barile, Elisa ^a   Chen, Vida ^a   Murphy, Ria ^a   Pellecchia, Maurizio ^a  

^a BURNHAM INSTITUTE   (United States)

^b INVITROGEN CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 (2,3 DIHYDROBENZO[B][1,4]DIOXIN 6 YL) 5 PHENYL 4H 1,2,4 TRIAZOL 3 YLTHIO] 5 NITROTHIAZOLE; 2 [4 (2,4 DICHLOROPHENYL) 5 (1 METHYL 1H PYRROL 2 YL) 4H 1,2,4 TRIAZOL 3 YLTHIO] 5 NITROTHIAZOLE; 2 [4 (3 METHOXYPHENYL) 5-PHENYL 4H 1,2,4 TRIAZOL 3 YLTHIO] 5 NITROTHIAZOLE; 2 [4 (FURAN 2 YLMETHYL) 5 (NAPHTHALEN 1 YL) 4H 1,2,4 TRIAZOL 3 YLTHIO] 5 NITROTHIAZOLE; 4 (2 METHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (2,4 DIMETHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (2,5 DIMETHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (3 FLUOROPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (3 METHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (3,4 DIFLUOROPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (3,4 DIMETHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (3,5 DIMETHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (4 FLUOROPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (4 METHOXYPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (4 NITROPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (4 TERT BUTYLPHENYL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (BENZO[D][1,3]DIOXOL 5 YL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 (NAPHTHALEN 1 YL) 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 4 CYCLOHEXYL 5 (5 NITROTHIAZOL 2 YLTHIO) 4H 1,2,4 TRIAZOL 3 OL; 5 (5 NITROTHIAZOL 2 YLTHIO) 4 [3 (TRIFLUOROMETHYL)PHENYL] 4H 1,2,4 TRIAZOL 3 OL; 5 (5 NITROTHIAZOL 2 YLTHIO) 4 [4 (TRIFLUOROMETHOXY)PHENYL] 4H 1,2,4 TRIAZOL 3 OL; 5 (5 NITROTHIAZOL 2 YLTHIO) 4 [4 (TRIFLUOROMETHYL)PHENYL] 4H 1,2,4 TRIAZOL 3 OL; 5 (5 NITROTHIOPHEN 2 YLTHIO) 4 PHENYL 4H 1,2,4-TRIAZOL 3 OL; 5 (BENZYLTHIO) 4 (2,3 DIHYDROBENZO[B][1,4]DIOXIN 6 YL) 4H 1,2,4-TRIAZOL 3 OL; 5 (BUTYLTHIO) 4 PHENYL 4H 1,2,4-TRIAZOL 3 OL; 5 (ETHYLTHIO) 4 PHENYL 4H 1,2,4-TRIAZOL 3 OL; STRESS ACTIVATED PROTEIN KINASE INHIBITOR; THIADIAZOLE DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; INSULIN SENSITIVITY; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ACTIVATING TRANSCRIPTION FACTOR 2; ANIMALS; BINDING SITES; DIABETES MELLITUS, TYPE 2; DRUG DESIGN; HELA CELLS; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN RESISTANCE; JNK MITOGEN-ACTIVATED PROTEIN KINASES; MALE; MICE; PHOSPHORYLATION; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; THIADIAZOLES; THIAZOLES; TRIAZOLES;

EID: 64549143360     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm801503n     Document Type: Article

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