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Synthesis and Structure-Activity Relationship of Salvinal Derivatives as Potent Microtubule Inhibitors.
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; Kuo, Yueh-Hsiung.
Afiliación
  • Chang CI; Department of Biological Science and Technology, National Pingtung University of Science and Technology, Pingtung 912, Taiwan.
  • Hsieh CC; Department of Pharmacy, Kaohsiung Veterans General Hospital, Kaohsiung 813, Taiwan.
  • Wein YS; School of Pharmacy and Institute of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan.
  • Kuo CC; Department of Chemistry, National Taiwan University, Taipei 114, Taiwan.
  • Chang CY; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli 350, Taiwan.
  • Lung J; Graduate Institute of Biomedical Sciences, China Medical University, Taichung 404, Taiwan.
  • Cherng JY; National Institute of Cancer Research, National Health Research Institutes, Miaoli 350, Taiwan.
  • Chu PC; Department of Medical Research and Development, Chiayi Chang Gung Memorial Hospital, Chiayi Branch, Chiayi 613, Taiwan.
  • Chang JY; Department of Chemistry and Biochemistry, National Chung Cheng University, Chiayi 613, Taiwan.
  • Kuo YH; Department of Cosmeceutics and Graduate Institute of Cosmeceutic, China Medical University, Taichung 404, Taiwan.
Int J Mol Sci ; 24(7)2023 Mar 28.
Article en En | MEDLINE | ID: mdl-37047358
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Int J Mol Sci Año: 2023 Tipo del documento: Article País de afiliación: Taiwán Pais de publicación: Suiza
Texto completo
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Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antineoplásicos Límite: Humans Idioma: En Revista: Int J Mol Sci Año: 2023 Tipo del documento: Article País de afiliación: Taiwán Pais de publicación: Suiza