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

Abstract:

:A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation with IC(50) value of 0.022 μM and showed 84% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.

journal_name

Bioorg Med Chem

authors

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

doi

10.1016/j.bmc.2011.03.008

subject

Has Abstract

pub_date

2011-04-15 00:00:00

pages

2633-40

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00189-1

journal_volume

19

pub_type

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