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<p>Lung cancer represents a substantial public health challenge, with NSCLC being the most prevalent subtype. There is an imperative need to enhance treatment strategies. The limited efficacy of conventional chemotherapy has prompted the investigation of alternative therapeutic approaches, highlighting the indispensable role of natural products and their structural modifications in drug development. This study presents new coumarin-based urea derivatives with potential for treating NSCLC. Among them, <b>6e</b> demonstrated significant inhibitory effects on A549 cells, with an IC<sub>50</sub> value of 3.50 μM. In vitro studies confirmed that <b>6e</b> effectively inhibited both the proliferation and migration of A549 cells, and significantly suppressed vascular tube formation, migration, and invasion in HUVECs through the inhibition of VEGFR signaling. Furthermore, in vivo studies revealed that <b>6e</b> effectively inhibited tumor growth and obstructed the metastatic process, while also exhibiting favorable safety profiles. These results support further development of coumarin-based urea derivatives as promising NSCLC therapies.</p><p></p>

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Synthesis and biological evaluation of coumarin-based urea derivatives demonstrating apoptosis-inducing and anti-angiogenic properties for non-small cell lung cancer treatment

  • 期刊论文

  • 发表日期：

    2025年12月5日

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  • Zirui Chen,
  • Qi Liao,
  • Pengyu Zhao,
  • Yuefei Geng,
  • Jianguo Wen,
  • Shu Liu,
  • Yanping Tang,
  • Chenjuan Zeng,
  • Tingting Yan,
  • Yongmei Shen,
  • Funeng Geng

摘要

Lung cancer represents a substantial public health challenge, with NSCLC being the most prevalent subtype. There is an imperative need to enhance treatment strategies. The limited efficacy of conventional chemotherapy has prompted the investigation of alternative therapeutic approaches, highlighting the indispensable role of natural products and their structural modifications in drug development. This study presents new coumarin-based urea derivatives with potential for treating NSCLC. Among them, 6e demonstrated significant inhibitory effects on A549 cells, with an IC50 value of 3.50 μM. In vitro studies confirmed that 6e effectively inhibited both the proliferation and migration of A549 cells, and significantly suppressed vascular tube formation, migration, and invasion in HUVECs through the inhibition of VEGFR signaling. Furthermore, in vivo studies revealed that 6e effectively inhibited tumor growth and obstructed the metastatic process, while also exhibiting favorable safety profiles. These results support further development of coumarin-based urea derivatives as promising NSCLC therapies.