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

Bioorganic and Medicinal Chemistry

Volumn 18, Issue 12, 2010, Pages 4459-4467

  Kim, Dae Kee ^a   Lee, Yeon Im ^a   Lee, Yeon Woo ^a   Dewang, Purushottam M ^a   Sheen, Yhun Yhong ^a   Kim, Yeo Woon ^a   Park, Hyun Ju ^b   Yoo, Jakyung ^b   Lee, Ho Soon ^c   Kim, Yong Kook ^c  

^a Ewha Womans University   (South Korea)

^b Sungkyunkwan University   (South Korea)

^c In2Gen Co Ltd   (South Korea)

Author keywords

ALK5 inhibitor; Cell based luciferase reporter assays; TGF

Indexed keywords

3 [[3 (6 METHYLPYRIDIN 2 YL) 4 (1,5 NAPHTHYRIDIN 2 YL) 1H PYRAZOL 1 YL]METHYL]BENZONITRILE; 3 [[3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOLIN 6 YL) 1H PYRAZOL 1 YL)METHYL)BENZONITRILE; 3 [[4 (6 METHYLPYRIDIN 2 YL) 3 (QUINOLIN 6 YL) 1H PYRAZOL 1 YL]METHYL]BENZONITRILE; 3 [[4 (6 METHYLPYRIDIN 2 YL) 5 (QUINOLIN 6 YL) 1H IMIDAZOL 2 YL]METHYL]BENZAMIDE; 3 [[4 (6 METHYLPYRIDIN 2 YL) 5 (QUINOLIN 6 YL) 1H IMIDAZOL 2 YL]METHYL]BENZONITRILE; 3 [[5 (6 METHYLPYRIDIN 2 YL) 4 (1,5 NAPHTHYRIDIN 2 YL) 1H IMIDAZOL 2 YL]METHYL]BENZAMIDE; 3 [[5 (6 METHYLPYRIDIN 2 YL) 4 (1,5 NAPHTHYRIDIN 2 YL) 1H IMIDAZOL 2 YL]METHYL]BENZONITRILE; 3 [[5 (6 METHYLPYRIDIN 2 YL) 4 (1,5 NAPHTHYRIDIN 2 YL) 1H PYRAZOL 1 YL]METHYL]BENZONITRILE; 3 [[5 (6 METHYLPYRIDIN 2 YL) 4 (QUINOLIN 6 YL) 1H PYRAZOL 1 YL]METHYL]BENZONITRILE; IMIDAZOLE DERIVATIVE; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1 KINASE INHIBITOR; UNCLASSIFIED DRUG; CYTOCHROME P450; IMIDAZOLE; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; PYRAZOLE DERIVATIVE; TGF-BETA TYPE I RECEPTOR; TRANSFORMING GROWTH FACTOR BETA RECEPTOR;

ARTICLE; CONTROLLED STUDY; DRUG METABOLISM; DRUG SYNTHESIS; ENZYME ASSAY; HUMAN; HUMAN CELL; IC 50; LIQUID CHROMATOGRAPHY; MOLECULAR DOCKING; MOLECULAR MODEL; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PROTEIN PHOSPHORYLATION; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; BINDING SITE; CELL LINE; CHEMISTRY; COMPUTER SIMULATION; ENZYME ACTIVE SITE; METABOLISM; SYNTHESIS;

BINDING SITES; CATALYTIC DOMAIN; CELL LINE; COMPUTER SIMULATION; CYTOCHROME P-450 ENZYME SYSTEM; HUMANS; IMIDAZOLES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES; RECEPTORS, TRANSFORMING GROWTH FACTOR BETA;

EID: 77953231559     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.04.071     Document Type: Article

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