2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-B1 and activin A signalling

Rudy Ciayadi, Mahesh Potdar, Kelly L. Walton, Craig A. Harrison, Geoffrey F. Kelso, Simon J. Harris, Milton T. W. Hearn

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    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 exhibited structural and functional attributes suitable for further investigation related to the development of more potent TGF-β inhibitors.
    Original languageEnglish
    Pages (from-to)5642-5645
    Number of pages4
    JournalBioorganic and Medicinal Chemistry Letters
    Issue number18
    Publication statusPublished - 2011


    • Transforming growth factor-β
    • activin A
    • low molecular weight inhibitors
    • structure-activity relationships
    • ATP-competitive ALK4/ALK5 inhibitors

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