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<p>Taiwanin A, a natural naphthalide lignan isolated from the heartwoods of <i>Taiwania cryptomerioides</i> Hayata, has previously been reported to have cytotoxicity against human tumor cells. In this study, a series of taiwanin A derivatives were synthesized and evaluated for their structure–activity relationship. Among the eleven taiwanin A derivatives, four compounds showed higher in vitro cytotoxic activity than taiwanin A. The biological evaluation of the synthesized compounds illustrated that the introduction of an electron-donating group in aryl ring A contributed to the antiproliferative potency, while in aryl ring B, it attenuated the cytotoxic activity. Compound <b>20</b> demonstrated excellent anticancer activity with an IC<sub>50</sub> value of 0.5 μM against HONE-1 human carcinoma cell lines, indicating that it could be a promising lead compound for further drug development studies.</p>

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Synthesis, Anticancer Evaluation and Structure–Activity Relationship of Taiwanin a Derivatives

  • 期刊论文

  • 发表日期：

    2025年1月1日

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  • Chi-I Chang,
  • Ching-Chuan Kuo,
  • Yung-Shung Wein,
  • Che-Yi Chao,
  • Yu-Chang Chen,
  • Jang-Yang Chang,
  • Yueh-Hsiung Kuo

摘要

Taiwanin A, a natural naphthalide lignan isolated from the heartwoods of Taiwania cryptomerioides Hayata, has previously been reported to have cytotoxicity against human tumor cells. In this study, a series of taiwanin A derivatives were synthesized and evaluated for their structure–activity relationship. Among the eleven taiwanin A derivatives, four compounds showed higher in vitro cytotoxic activity than taiwanin A. The biological evaluation of the synthesized compounds illustrated that the introduction of an electron-donating group in aryl ring A contributed to the antiproliferative potency, while in aryl ring B, it attenuated the cytotoxic activity. Compound 20 demonstrated excellent anticancer activity with an IC50 value of 0.5 μM against HONE-1 human carcinoma cell lines, indicating that it could be a promising lead compound for further drug development studies.