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 …

…, M Krishnaiah, D Sreenu, VB Subrahmanyam…

Index: Jin, Cheng Hua; Krishnaiah, Maddeboina; Sreenu, Domalapally; Subrahmanyam, Vura Bala; Rao, Kota Sudhakar; Mohan, Annaji Venkata Nagendra; Park, Chul-Yong; Son, Jee-Yeon; Sheen, Yhun Yhong; Kim, Dae-Kee Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 20 p. 6049 - 6053

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Citation Number: 16

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 IC50 value of 0.57 ...