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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-beta type 1 receptor kinase inhibitors

Authors
 Maddeboina Krishnaiah  ;  Cheng Hua Jin  ;  Domalapally Sreenu  ;  Vura Bala Subrahmanyama  ;  Kota Sudhakar Rao  ;  Do-Hyun Son  ;  Hyun-Ju Park  ;  Seung Won Kim  ;  Yhun Yhong Sheen  ;  Dae-Kee Kim 
Citation
 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, Vol.57 : 74-84, 2012 
Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN
 0223-5234 
Issue Date
2012
MeSH
Cell Line, Transformed ; Enzyme Assays ; Genes, Reporter ; Humans ; Keratinocytes/drug effects* ; Keratinocytes/enzymology ; Luciferases ; Molecular Docking Simulation ; Phosphorylation ; Protein Kinase Inhibitors/chemistry* ; Protein Kinase Inhibitors/pharmacology ; Protein-Serine-Threonine Kinases/antagonists & inhibitors ; Protein-Serine-Threonine Kinases/chemistry* ; Receptors, Transforming Growth Factor beta/antagonists & inhibitors ; Receptors, Transforming Growth Factor beta/chemistry* ; Structure-Activity Relationship ; Thiazoles/chemical synthesis* ; Thiazoles/pharmacology ; Transfection
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 IC(50) 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.
Full Text
https://www.sciencedirect.com/science/article/pii/S0223523412005508
DOI
10.1016/j.ejmech.2012.09.011
Appears in Collections:
1. College of Medicine (의과대학) > Others (기타) > 1. Journal Papers
Yonsei Authors
Kim, Seung Won(김승원) ORCID logo https://orcid.org/0000-0002-1692-1192
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/158295
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