Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin- 2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

European Journal of Medicinal Chemistry

Volumn 46, Issue 9, 2011, Pages 3917-3925

  Jin, Cheng Hua ^a   Sreenu, Domalapally ^a   Krishnaiah, Maddeboina ^a   Subrahmanyam, Vura Bala ^a   Rao, Kota Sudhakar ^a   Nagendra Mohan, Annaji Venkata ^a   Park, Chul Yong ^a   Son, Jee Yeon ^a   Son, Do Hyun ^b   Park, Hyun Ju ^b   Sheen, Yhun Yhong ^a   Kim, Dae Kee ^a  

^a Ewha Womans University   (South Korea)

^b Sungkyunkwan University   (South Korea)

Author keywords

ALK5 inhibitor; Cancer; Cell based luciferase reporter assay; Docking; Fibrosis; Kinase assay; TGF

Indexed keywords

1 (6 METHYLPYRIDIN 2 YL) 2 (QUINOXALIN 6 YL)ETHANONE; 2 (2,3 DIMETHYLQUINOXALIN 6 YL) 1 (6 METHYLPYRIDIN 2 YL)ETHANO; 2 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]N PHENYLACETAMIDE; 2 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]N PHENYLETHANETHIOAMIDE; 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]N PHENYLACETAMIDE; 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]N PHENYLETHANETHIOAMIDE; 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 5 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]N PHENYLACETAMIDE; 2 [5 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]N PHENYLACETAMIDE; 2,3 DIMETHYL 6 [3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 4 YL]QUINOXALINE; 3 [2 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]ACETAMIDO]BENZAMIDE; 3 [2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]ACETAMIDO]BENZAMIDE; 3 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]N PHENYLPROPANAMIDE; 3 BROMO N(3 CYANOPHENYL)PROPANAMIDE; 6 [3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 4 YL]QUINOXALINE; A 83 01; ENZYME INHIBITOR; GW 6604; IN 1130; IN 1233; LY 2157299; MITOGEN ACTIVATED PROTEIN KINASE P38; N (3 CYANOPHENYL) 2 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]; N (3 CYANOPHENYL) 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]ACETAMIDE; N (3 CYANOPHENYL) 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 5 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]ACETAMIDE; N (3 CYANOPHENYL) 2 [5 (6 METHYPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YL]ACETAMIDE; N (3 CYANOPHENYL) 3 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YLPROPANAMIDE; N(3 CYANOPHENYL) 2 [3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOXALIN 6 YL) 1H PYRAZOL 1 YLETHANETHIOAMIDE; N(3 CYANOPHENYL) 2 [4 (2,3 DIMETHYLQUINOXALIN 6 YL) 3 (6 METHYLPYRIDIN 2 YL) 1H PYRAZOL 1 YL]ETHANETHIOAMIDE; PYRAZOLE DERIVATIVE; SB 505124; SB 525234; SD 208; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1 INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG BINDING; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME ASSAY; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; EVALUATION; IC 50; SUBSTITUTION REACTION;

ANIMALS; CELL LINE; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES; RECEPTORS, TRANSFORMING GROWTH FACTOR BETA; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; X-RAY DIFFRACTION;

EID: 80052951712     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2011.05.063     Document Type: Article

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