Biological Evaluation and SAR Analysis of O‐Methylated Analogs of Quercetin as Inhibitors of Cancer Cell Proliferation |
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| Authors: | Zhi‐Hao Shi Nian‐Guang Li Yu‐Ping Tang Qian‐Ping Shi Hao Tang Wei Li Xu Zhang Hai‐An Fu Jin‐Ao Duan |
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| Affiliation: | 1. National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, China;2. Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu, China;3. Department of Pharmacology, Emory University School of Medicine, Atlanta, GA, United States |
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| Abstract: | Using a high‐throughout screening approach, the anticancer activities of 16 O‐methylated (OMe) analogs of quercetin were assessed. The structure–activity relationships showed that OMe moieties at the 4′ and/or 7 positions were important for maintaining inhibitory activities against the 16 cancer cell lines. Furthermore, when the OH groups at the 3′ and 4′ positions were both replaced by OMe moieties, anticancer activity was enhanced. |
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| Keywords: | structure– activity relationship quercetin methylation analog anticancer |
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