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<p>A series of <i>N</i>′-aryldenehydrazide derivatives from isopimaric acid were designed, synthesized, and evaluated for their anticancer activities. Some synthesized compounds showed stronger anticancer activity than the positive control drug 5-fluorouracil (5-FU). Compound <b>3c</b>, with a hydroxyl and a methoxyl in the benzene, exhibited the strongest cytotoxicity against human malignant melanoma cells (A375) and ovarian carcinoma cells (ES-2), with IC<sub>50</sub> values of 9.54 and 5.43 μM, respectively. It also demonstrated reduced toxicity to normal human hepatocytes (L-O2), making it the most promising anticancer candidate. Structure–activity relationship studies revealed that the introduction of the hydroxyl group into the benzene ring is beneficial to improve the antitumor activity.</p>

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Design, Synthesis, and Anticancer Activity Evaluation of N′-Arylidenehydrazides of Isopimaric Acid

  • 期刊论文

  • 发表日期：

    2025年11月19日

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  • Juan-Juan Liu,
  • Ya Gao,
  • Zhen-Dong Zhao,
  • Guo-Yong Luo,
  • Shao-Ping Yang

摘要

A series of N′-aryldenehydrazide derivatives from isopimaric acid were designed, synthesized, and evaluated for their anticancer activities. Some synthesized compounds showed stronger anticancer activity than the positive control drug 5-fluorouracil (5-FU). Compound 3c, with a hydroxyl and a methoxyl in the benzene, exhibited the strongest cytotoxicity against human malignant melanoma cells (A375) and ovarian carcinoma cells (ES-2), with IC50 values of 9.54 and 5.43 μM, respectively. It also demonstrated reduced toxicity to normal human hepatocytes (L-O2), making it the most promising anticancer candidate. Structure–activity relationship studies revealed that the introduction of the hydroxyl group into the benzene ring is beneficial to improve the antitumor activity.