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

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

  • Bioorg Med Chem Lett. 2011 Sep 15;21(18):5642-5. doi: 10.1016/j.bmcl.2010.12.120.
Rudy Ciayadi 1,  Mahesh Potdar,  Kelly L Walton,  Craig A Harrison,  Geoffrey F Kelso,  Simon J Harris,  Milton T W Hearn
Affiliations

Affiliation

  • 1 Centre for Green Chemistry, Monash University, Clayton, Victoria 3800, Australia.
PMID: 21783359 DOI: 10.1016/j.bmcl.2010.12.120
Abstract

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.

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