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<p>In the current work, we carried out the synthesis and evaluation of coumarin derivatives <b>4a–f</b> (R= hydrogen, fluoro, bromo, methoxy, trifluoromethyl) against their TGF-β1 inhibitory activity. EIA kits were used to detect the in vitro inhibitory activity of human TGF-β1 for <b>4a–f</b> following the manufacturer’s instructions. Among them, compound <b>4f</b> exhibited the strongest activity with an IC<sub>50</sub> value of 6.43 μM, making its potency comparable to the positive control, coumarin (IC<sub>50</sub> = 7.81 μM).</p>

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Synthesis and Biological Evaluation of Coumarin Derivatives as Potent TGF-β1 Inhibitors

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • Kechong Fan,
  • Yang Liu,
  • Yan Tian,
  • Wei Wang,
  • Xue Hu,
  • Luping Wang,
  • Fenglin Zhang

摘要

In the current work, we carried out the synthesis and evaluation of coumarin derivatives 4a–f (R= hydrogen, fluoro, bromo, methoxy, trifluoromethyl) against their TGF-β1 inhibitory activity. EIA kits were used to detect the in vitro inhibitory activity of human TGF-β1 for 4a–f following the manufacturer’s instructions. Among them, compound 4f exhibited the strongest activity with an IC50 value of 6.43 μM, making its potency comparable to the positive control, coumarin (IC50 = 7.81 μM).