Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

被引：88

作者：

Kim, DK

Kim, J

Park, HJ

机构：

[1] Ewha Womans Univ, Coll Pharm, Seoul 120750, South Korea

[2] Sungkyunkwan Univ, Coll Pharm, Suwon 440746, Kyungkido, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 10期

关键词：

2-pyridinyl-[1,2,3]triazoles; inhibitors; TGF-beta; 1; type; receptor; ALK5;

D O I：

10.1016/j.bmcl.2004.03.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 muM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38alpha MAP kinase inhibition (13%) at a concentration of 10 muM that is much lower than that of SB-431542 (54%). (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2401 / 2405

页数：5

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