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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

Title
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
Authors
Jin C.H.Sreenu D.Krishnaiah M.Subrahmanyam V.B.Rao K.S.Nagendra Mohan A.V.Park C.-Y.Son J.-Y.Son D.-H.Park H.-J.Sheen Y.Y.Kim D.-K.
Ewha Authors
신윤용김대기
SCOPUS Author ID
신윤용scopus; 김대기scopus
Issue Date
2011
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 46, no. 9, pp. 3917 - 3925
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl) pyrazoles 14a-d, 15a-d, 17a, 17b, 18a-d, 19a, and 19b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 2-[3-(6-methylpyridin-2-yl)-4- (quinoxalin-6-yl)-1H-pyrazol-1-yl]-N-phenylethanethioamide (18a) inhibited ALK5 phosphorylation with an IC 50 value of 0.013 μM and showed 80% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2011 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2011.05.063
Appears in Collections:
약학대학 > 약학과 > Journal papers
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