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Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-β type1 receptor kinase inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Mar2008, Vol. 18 Issue 6, p2122-2127. 6p. - Publication Year :
- 2008
-
Abstract
- Abstract: A series of 5-(pyridin-2-yl)thiazoles (14a–l and 15a–l) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-[[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl]benzamide (15i) and 3-[[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl]benzamide (15k) showed more than 95% inhibition at 0.1μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luciferase reporter construct. [Copyright &y& Elsevier]
- Subjects :
- *CYTOKINES
*BENZAMIDE
*AMIDES
*GROWTH factors
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 18
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 31303718
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.084