Synthesis and Structure–Activity Relationship of Salvinal Derivatives as Potent Microtubule Inhibitors

Chi I. Chang, Cheng Chih Hsieh, Yung Shung Wein, Ching Chuan Kuo, Chi Yen Chang, Jrhau Lung, Jong Yuh Cherng, Po Chen Chu, Jang Yang Chang, Yueh Hsiung Kuo

Research output: Contribution to journalArticlepeer-review


Salvinal is a natural lignan isolated from the roots of Salvia mitorrhiza 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 25 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 25 showed depolymerization activity in a dose-dependent manner. Our findings indicate that compound 25 is a promising anticancer agent with depolymerization activity that has potential for the management of malignance.

Original languageEnglish
Article number6386
JournalInternational journal of molecular sciences
Issue number7
Publication statusPublished - Apr 2023


  • anticancer
  • lignan
  • microtubule depolymerization
  • Salvia mitorrhiza
  • salvinal

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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