1. Synthesis and Structure–Activity Relationship of Salvinal Derivatives as Potent Microtubule Inhibitors.
- Author
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Chang, Chi-I, Hsieh, Cheng-Chih, Wein, Yung-Shung, Kuo, Ching-Chuan, Chang, Chi-Yen, Lung, Jrhau, Cherng, Jong-Yuh, Chu, Po-Chen, Chang, Jang-Yang, and Kuo, Yueh-Hsiung
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STRUCTURE-activity relationships , *MICROTUBULES , *CELL lines , *ANTINEOPLASTIC agents , *SALVIA miltiorrhiza , *NEOLIGNANS - Abstract
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. [ABSTRACT FROM AUTHOR]
- Published
- 2023
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