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Salvinal is a natural lignan isolated from the roots of <i>Salvia mitorrhiza</i> Bunge (Danshen). Previous studies have demonstrated its anti-proliferative activity in both drug-sensitive and -resistant cancer cell lines, with IC₅₀ values ranging from 4–17 µM. In this study, a series of salvinal derivatives was synthesized and evaluated for the structure–activity relationship. Among the twenty-four salvinal derivatives, six compounds showed better anticancer activity than salvinal. Compound <b>25</b> displayed excellent anticancer activity, with IC₅₀ values of 0.13–0.14 µM against KB, KB-Vin10 (overexpress MDR/Pgp), and KB-7D (overexpress MRP) human carcinoma cell lines. Based on our in vitro microtubule depolymerization assay, compound <b>25</b> showed depolymerization activity in a dose-dependent manner. Our findings indicate that compound <b>25</b> is a promising anticancer agent with depolymerization activity that has potential for the management of malignance.