2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl) pyridines as inhibitors of TGF-β1 and activin A signalling

R Ciayadi, M Potdar, KL Walton, CA Harrison…

文献索引：Ciayadi, Rudy; Potdar, Mahesh; Walton, Kelly L.; Harrison, Craig A.; Kelso, Geoffrey F.; Harris, Simon J.; Hearn, Milton T.W. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5642 - 5645

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被引用次数: 8

摘要

Novel inhibitors of TGF-β1 and activin A signalling based on a 2-aryl-4-(3-(pyridin-2-yl)-1H- pyrazol-4-yl) pyridine pharmacophore have been synthesised. Compounds containing phenyl or aromatic nitrogen heterocycle substituents inhibited both types of signalling with HEK-293T cells in culture, with a selectivity preference for TGF-β1. Synthetic compounds containing pyridin-3-yl, pyrazol-4-yl, pyrazol-1-yl or 1H-imidazoyl-1-yl substituents ...