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Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin- 2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title
Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin- 2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors
Authors
Krishnaiah M.Jin C.H.Sreenu D.Subrahmanyam V.B.Rao K.S.Son D.-H.Park H.-J.Kim S.W.Sheen Y.Y.Kim D.-K.
Ewha Authors
신윤용김대기김승원
SCOPUS Author ID
신윤용scopus; 김대기scopus
Issue Date
2012
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 57, pp. 74 - 84
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4] triazolo[1,5-a]pyridin-6-yl)thiazoles 12a-ab, 13a, 13b, and 18a-d has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The N-(3-fluorobenzyl)-4-(6- methylpyridin-2-yl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiazol-2-amine (12b) inhibited ALK5 phosphorylation with an IC50 value of 7.01 nM and showed 61% inhibition at 30 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2012 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2012.09.011
Appears in Collections:
약학대학 > 약학과 > Journal papers
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