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Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Abstract：

:A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-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-([1,2,4]triazolo[1,5-a]pyridin-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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Jin CH,Krishnaiah M,Sreenu D,Subrahmanyam VB,Rao KS,Mohan AV,Park CY,Son JY,Sheen YY,Kim DK

doi

10.1016/j.bmcl.2011.08.064

subject

Has Abstract

pub_date

2011-10-15 00:00:00

pages

6049-53

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01160-7

journal_volume

21

pub_type

杂志文章

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