2. Academic Validation
  3. Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring

Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring

  • Bioorg Med Chem Lett. 2012 May 15;22(10):3392-7. doi: 10.1016/j.bmcl.2012.04.013.
Mark L Boys 1,  Feng Bian,  James B Kramer,  Christopher L Chio,  Xiao-Dan Ren,  Huifen Chen,  Stephen D Barrett,  Karen E Sexton,  Donna M Iula,  Gary F Filzen,  Maria N Nguyen,  Paul Angell,  Victoria L Downs,  Zhi Wang,  Neil Raheja,  Edmund L Ellsworth,  Stephen Fakhoury,  Larry D Bratton,  Paul R Keller,  Richard Gowan,  Elena M Drummond,  Samarendra N Maiti,  Mostofa A Hena,  Leroy Lu,  Patrick McConnell,  John D Knafels,  Venkataraman Thanabal,  Fang Sun,  Diane Alessi,  Ann McCarthy,  Erli Zhang,  Barry C Finzel,  Sneha Patel,  Susan M Ciotti,  Rone Eisma,  N A Payne,  Richard B Gilbertsen,  Catherine R Kostlan,  David J Pocalyko,  Deepak S Lala
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Ann Arbor Laboratories, Ann Arbor, MI 48105, USA. mark.boys@arraybiopharma.com
PMID: 22542194 DOI: 10.1016/j.bmcl.2012.04.013
Abstract

A series of 2-(1H-pyrazol-1-yl)pyridines are described as inhibitors of ALK5 (TGFβ receptor I kinase). Modeling compounds in the ALK5 kinase domain enabled some optimization of potency via substitutions on the pyrazole core. One of these compounds PF-03671148 gave a dose dependent reduction in TGFβ induced fibrotic gene expression in human fibroblasts. A similar reduction in fibrotic gene expression was observed when PF-03671148 was applied topically in a rat wound repair model. Thus these compounds have potential utility for the prevention of dermal scarring.

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