Bioorganic & medicinal chemistry, 2011-04, Vol.19 (8), p.2633-2640
2011
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry, 2011-04, Vol.19 (8), p.2633-2640
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- Elsevier ScienceDirect Journals
- Beschreibungen/Notizen
- A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles 14a– e, 15a– e, 17a– c, and 18a– d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation with IC 50 value of 0.022 μM and showed 84% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2011.03.008Titel-ID: cdi_proquest_miscellaneous_861789267
- Format
- –
- Schlagworte
- ALK5 inhibitor, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, Cancer, Cell Line, Cell-based luciferase reporter assay, enzyme activity, Enzyme Assays, Fibrosis, Humans, inhibitory concentration 50, Kinase assay, luciferase, Medical sciences, Miscellaneous, Pharmacology. Drug treatments, phosphorylation, Phosphorylation - drug effects, Protein Kinase Inhibitors - chemical synthesis, Protein Kinase Inhibitors - pharmacology, Protein-Serine-Threonine Kinases - antagonists & inhibitors, Protein-Serine-Threonine Kinases - metabolism, pyrazoles, Pyrazoles - chemical synthesis, Pyrazoles - pharmacology, Receptors, Transforming Growth Factor beta - antagonists & inhibitors, Receptors, Transforming Growth Factor beta - metabolism, Structure-Activity Relationship, TGF-β