Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 205, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112663
Keywords
Mannich base; Semisynthesis; Magnolol derivative; Anti-cancer; Autophagy
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Funding
- Science and Technology Development Fund, Macau SAR [0074/2019/AMJ, 0004/2019/A1, 0023/2019/AKP]
- Department of Science and Technology of Guangdong Province, China
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Magnolol, a natural bioactive neolignan, was found in the bark of a traditional Chinese medicine Magnoliae officinalis (Hou Po in Chinese). In this study, thrity-two magnolol-based Mannich base derivatives 3a-p and 4a-p were synthesized, and evaluated for their anti-proliferative activities against a panel of human tumor cell lines (T47D, MCF-7, Hela and A549). Among all derivatives, compound 3p displayed the most potent antiproliferative activity against T47D, MCF-7 and Hela cell lines with IC50 values of 0.91, 3.32 and 1.71 mu M, respectively. Compared with the parental magnolol and the positive drug cisplatin, 3p exhibited up to 76.1-fold and 10.3-fold enhancement of cytotoxic effect on T47D cancer cells, respectively. Mechanism study revealed that the most potent derivative 3p suppressed cancer cells via inducing autophagy. Moreover, 3p also possessed suppressive effects on migration of T47D and Hela cancer cells. In addition, some interesting structure-activity relationships (SARs) were also summarized. (C) 2020 Elsevier Masson SAS. All rights reserved.
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