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<p>Formononetin, derived from <i>Orostachys japonica</i> (a traditional Chinese medicine), has been reported to have anti-cancer activity. In continuation of work on the exploration of formononetin derivative development, we designed and synthesized a novel series of formononetin-piperazine hybrids as anticancer agents, followed by evaluation of their antiproliferative activities against three cancer cell lines. Among these derivatives, compounds <b>6g</b> (IC<sub>50</sub> = 5.87 ± 0.96 μM) and <b>6h</b> (IC<sub>50</sub> = 3.50 ± 0.65 μM) emerged as the most potent analogues, demonstrating the best inhibitory activities against MGC-803 human gastric cancer cells. The structure-activity relationships (SARs) indicated that the introduction of substituents at meta-position of piperazine-linked phenyl moiety was helpful to enhance the anticancer potency. Further mechanistic investigations revealed that <b>6g</b> and <b>6h</b> exerted multimodal antitumor effects through G2/M phase arrest induction, apoptosis promotion, and migration suppression in MGC-803 cells. Thus, <b>6g</b> and <b>6h</b> could be deeply developed for the development of formononetin-based anti-cancer candidates.</p>

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Design and synthesis of formononetin-piperazine hybrids that inhibit the migration and growth of MGC-803 cells

  • 期刊论文

  • 发表日期：

    2025年6月6日

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  • Ya Wang,
  • Yan Jin,
  • Jian Song,
  • Sai-Yang Zhang,
  • Wang Wang,
  • Yan Xu,
  • Hong-Ju Liu

摘要

Formononetin, derived from Orostachys japonica (a traditional Chinese medicine), has been reported to have anti-cancer activity. In continuation of work on the exploration of formononetin derivative development, we designed and synthesized a novel series of formononetin-piperazine hybrids as anticancer agents, followed by evaluation of their antiproliferative activities against three cancer cell lines. Among these derivatives, compounds 6g (IC50 = 5.87 ± 0.96 μM) and 6h (IC50 = 3.50 ± 0.65 μM) emerged as the most potent analogues, demonstrating the best inhibitory activities against MGC-803 human gastric cancer cells. The structure-activity relationships (SARs) indicated that the introduction of substituents at meta-position of piperazine-linked phenyl moiety was helpful to enhance the anticancer potency. Further mechanistic investigations revealed that 6g and 6h exerted multimodal antitumor effects through G2/M phase arrest induction, apoptosis promotion, and migration suppression in MGC-803 cells. Thus, 6g and 6h could be deeply developed for the development of formononetin-based anti-cancer candidates.