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

…, D Sreenu, M Krishnaiah, VB Subrahmanyam…

Index: Jin, Cheng Hua; Sreenu, Domalapally; Krishnaiah, Maddeboina; Subrahmanyam, Vura Bala; Rao, Kota Sudhakar; Nagendra Mohan, Annaji Venkata; Park, Chul-Yong; Son, Jee-Yeon; Son, Do-Hyun; Park, Hyun-Ju; Sheen, Yhun Yhong; Kim, Dae-Kee European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 3917 - 3925

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Citation Number: 13

Abstract

A series of 1-substituted-3 (5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl) pyrazoles 14a–d, 15a–d, 17a, 17b, 18a–d, 19a, and 19b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 2-[3- (6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-pyrazol-1-yl]-N-phenylethanethioamide (18a) inhibited ALK5 phosphorylation with an IC50 value of 0.013 μM and showed 80% ...