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<p>Eleven novel C-16 triazole-fused isosteviol derivatives <b>6a–6k</b> were synthesized by “Huisgen-click” 1,3-dipolar cycloaddition reaction. The structures of synthesized compounds were characterized by IR, NMR, and HR-MS spectra, respectively. Furthermore, the anti-LSD1 activity of compounds was investigated, after which the results revealed that compound <b>6h</b> exhibited the best inhibitory activity with an IC<sub>50</sub> value of 8.944 ± 1.013 μM. The structure–activity relationships were further analyzed to guide the future design of novel isosteviol derivatives with enhanced LSD1 inhibitory capabilities.</p>

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Synthesis, Structure, and Anti-LSD1 Activity of Novel C-16 Triazole-Fused Isosteviol Derivatives

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • Cong-Jun Liu,
  • Wen-Shuo Jiang,
  • Wei-Wen Huang,
  • Ke-Jia Qiang,
  • Shang-Yu Yang,
  • Li-Na Liu,
  • Wen-Min Zhang,
  • Yu-Ling Li,
  • Yu-Tao Min,
  • Yang Sun,
  • Yu-Fei Wang

摘要

Eleven novel C-16 triazole-fused isosteviol derivatives 6a–6k were synthesized by “Huisgen-click” 1,3-dipolar cycloaddition reaction. The structures of synthesized compounds were characterized by IR, NMR, and HR-MS spectra, respectively. Furthermore, the anti-LSD1 activity of compounds was investigated, after which the results revealed that compound 6h exhibited the best inhibitory activity with an IC50 value of 8.944 ± 1.013 μM. The structure–activity relationships were further analyzed to guide the future design of novel isosteviol derivatives with enhanced LSD1 inhibitory capabilities.