Synthesis and biological evaluation of 1, 2, 4-trisubstituted imidazoles and 1, 3, 5-trisubstituted pyrazoles as inhibitors of transforming growth factor β type 1 receptor ( …

X Li, L Wang, L Long, J Xiao, Y Hu, S Li

Index: Li, Xingzhou; Wang, Lili; Long, Long; Xiao, Junhai; Hu, Yuandong; Li, Song Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4868 - 4872

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Citation Number: 20

Abstract

Two series of nitrogenous heterocycle compounds—1, 2, 4-trisubstituted imidazoles and 1, 3, 5-trisubstituted pyrazoles have been synthesized and evaluated for their ALK5 inhibitory activity and cytotoxicity in TGFβ-Smad2 assay and MTT assay, respectively. The ALK4/5/7 inhibitory activity of some compound was also evaluated in ALK4/5/7 autophosphorylation assays. Compounds 6c and 14c showed relatively potent ALK5 inhibition while weak ...