ArticleMolecules (Basel, Switzerland)2012
Design, synthesis and anti-fibrosis activity study of N₁-substituted phenylhydroquinolinone derivatives.
Article in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 15 citations in OpenAlex.
- Fluorofenidone ameliorates pressure overload-induced heart failure by stabilizing SERCA2a in male mice.Nature communications · 2026Article
- Hydronidone Mitigates Pulmonary Fibrosis by Regulating the TGF-β/Smad2/3 Axis inACS pharmacology & translational science · 2025Article
- Design and Synthesis of Novel Pirfenidone Analogues for Targeting Fibroblast Differentiation via Transforming Growth Factor-β/Smad Pathway UsingACS pharmacology & translational science · 2025Article
- Synthesis and structure-activity relationships of pirfenidone derivatives as anti-fibrosis agentsRSC medicinal chemistry · 2022Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pirfenidone (5-methyl-1-phenyl-2(1H)-pyridone, PFD) is a small-molecule compound acting on multiple targets involved in pathological fibrogenesis and is effective to increase the survival of patients with fibrosis, such as idiopathic pulmonary fibrosis. However, PFD is not active enough, requiring a high daily dose. In this study, to keep the multiple target profiles, N₁-substituted phenylhydroquinolinone derivatives, which retain the 1-phenyl-2(1H)-pyridone scaffold were designed and synthesized. The preliminary anti-fibrosis activities for all target compounds were evaluated on a NIH3T3 fibroblast cell line using MTT assay methods. Most compounds showed significant inhibition on NIH3T3 cell proliferation with a IC₅₀ range of 0.09-26 mM, among which 5-hydroxy-1-(4'-bromophenyl)-5,6,7,8-tetrahydroquinolin-2(1H)-one (6j) displayed 13 times higher potency (IC₅₀ = 0.3 mM) than that of AKF-PD (IC₅₀ = 4.2 mM). These results suggest that N₁-substituted phenylhydroquinolinone is a promising scaffold which can be applied for further investigation and for developing novel anti-fibrosis agents.
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