Title of article
Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
Author/Authors
Dae-Kee Kim، نويسنده , , Joonseop Kim، نويسنده , , Hyun Ju Park، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
2401
To page
2405
Abstract
A series of 2-pyridinyl-[1,2,3]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 inhibition (SBE-luciferase activity, 25%; p3TP-luciferase activity, 17%) at a concentration of 5 μM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38α MAP kinase inhibition (13%) at a concentration of 10 μM that is much lower than that of SB-431542 (54%).
Keywords
ALK5. , 3]triazoles , 2 , inhibitors , TGF-b1 type 1 receptor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794407
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