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<p>To investigate the impact of C3-methyl substitution of naphtho[1,2-<i>b</i>]furan-4,5-dione analogs on antitumor efficacy, 16 NQO1 substrate analogs of C3-methylated (<b>TC1–TC8</b>) and C3-demethylated (<b>TC1</b>′<b>–TC8</b>′) were synthesized. The anticancer activities against K562, LNCaP, HeLa, and MDA-MB-231 suggested that methyl and demethyl derivatives of naphtho[1,2-<i>b</i>]furan-4,5-dione analogs have comparable cytotoxicity and this value depends more on the nature of the substituent at position C-2.</p>

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Investigating the Impact of C3-Methyl of Naphtho[1,2-b]Furan-4,5-Dione Analogs for Anticancer Activity

  • 期刊论文

  • 发表日期：

    2025年9月18日

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  • Yue Zhu,
  • Jia Yu,
  • Xin Tan,
  • Ni Zhang,
  • Jin-Yu Li,
  • Hua-Yong Lou,
  • Heng Luo,
  • Chao Chen,
  • Wei-Dong Pan

摘要

To investigate the impact of C3-methyl substitution of naphtho[1,2-b]furan-4,5-dione analogs on antitumor efficacy, 16 NQO1 substrate analogs of C3-methylated (TC1–TC8) and C3-demethylated (TC1′–TC8′) were synthesized. The anticancer activities against K562, LNCaP, HeLa, and MDA-MB-231 suggested that methyl and demethyl derivatives of naphtho[1,2-b]furan-4,5-dione analogs have comparable cytotoxicity and this value depends more on the nature of the substituent at position C-2.