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 mu M against HONE-1 human carcinoma cell lines, indicating that it could be a promising lead compound for further drug development studies.
Date:
2025-02-03
Relation:
Chemistry of Natural Compounds. 2025 Feb 03;61:11-18.
