@article{09e488f9d93e4920b868b510755e6886,
title = "Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring",
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.",
keywords = "Activin receptor-like Kinase 5, Dermal scarring, Topical, Transforming growth factor beta, Wound repair",
author = "Boys, {Mark L.} and Feng Bian and Kramer, {James B.} and Chio, {Christopher L.} and Ren, {Xiao Dan} and Huifen Chen and Barrett, {Stephen D.} and Sexton, {Karen E.} and Iula, {Donna M.} and Filzen, {Gary F.} and Nguyen, {Maria N.} and Paul Angell and Downs, {Victoria L.} and Zhi Wang and Neil Raheja and Ellsworth, {Edmund L.} and Stephen Fakhoury and Bratton, {Larry D.} and Keller, {Paul R.} and Richard Gowan and Drummond, {Elena M.} and Maiti, {Samarendra N.} and Hena, {Mostofa A.} and Leroy Lu and Patrick McConnell and Knafels, {John D.} and Venkataraman Thanabal and Fang Sun and Diane Alessi and Ann McCarthy and Erli Zhang and Finzel, {Barry C.} and Sneha Patel and Ciotti, {Susan M.} and Rone Eisma and Payne, {N. A.} and Gilbertsen, {Richard B.} and Kostlan, {Catherine R.} and Pocalyko, {David J.} and Lala, {Deepak S.}",
year = "2012",
month = may,
day = "15",
doi = "10.1016/j.bmcl.2012.04.013",
language = "English (US)",
volume = "22",
pages = "3392--3397",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "10",
}
