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Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2- yl)-4-([1,2,4triazolo[1,5-apyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors
- Title
- Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2- yl)-4-([1,2,4triazolo[1,5-apyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors
- Authors
- Jin C.H.; Krishnaiah M.; Sreenu D.; Subrahmanyam V.B.; Rao K.S.; Mohan A.V.N.; Park C.-Y.; Son J.-Y.; Sheen Y.Y.; Kim D.-K.
- Ewha Authors
- 신윤용; 김대기
- SCOPUS Author ID
- 신윤용; 김대기
- Issue Date
- 2011
- Journal Title
- Bioorganic and Medicinal Chemistry Letters
- ISSN
- 0960-894X
- Citation
- Bioorganic and Medicinal Chemistry Letters vol. 21, no. 20, pp. 6049 - 6053
- Indexed
- SCI; SCIE; SCOPUS
- Document Type
- Article
- Abstract
- A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4triazolo[1,5- apyridin-6-yl)pyrazoles 14a-ae, 16a, 16b, and 21a-c has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 4-([1,2,4triazolo[1,5-apyridin-6-yl)- N-(4-methoxyphenyl)-3-(6-methylpyridin-2-yl)-1H-pyrazole-1-carbothioamide (14n) inhibited ALK5 phosphorylation with IC 50 value of 0.57 nM and showed 94% inhibition at 100 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2011 Elsevier Ltd. All rights reserved.
- DOI
- 10.1016/j.bmcl.2011.08.064
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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