Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives
AbstractA one-step synthesis of phloretin derivatives 2–11 from phloretin in good to excellent yields is reported. Their structures were characterized by 1H-NMR, 13C-NMR and MS, and the structures of 8 and 11 were determined by X-ray diffraction analysis. A mechanism for the formation of 9–11 is proposed. Compared with the anticancer drug docetaxel, phloretin, phloretin derivatives and phlorizin exhibited moderate cytotoxicity toward the MDA-MB-231, SPC-A1, A549, MCF-7 and EC109 cell lines. Among all of the tested compounds, 7 exhibited the strongest cytotoxicity toward the five cell lines and was more active than docetaxel in MDA-MB-231 cells. Our findings suggest that these derivatives hold great promise for further development as anticancer agents. View Full-Text
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Wang, L.; Li, Z.-W.; Zhang, W.; Xu, R.; Gao, F.; Liu, Y.-F.; Li, Y.-J. Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives. Molecules 2014, 19, 16447-16457.
Wang L, Li Z-W, Zhang W, Xu R, Gao F, Liu Y-F, Li Y-J. Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives. Molecules. 2014; 19(10):16447-16457.Chicago/Turabian Style
Wang, Li; Li, Zheng-Wei; Zhang, Wei; Xu, Rui; Gao, Fei; Liu, Yang-Feng; Li, Ya-Jun. 2014. "Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives." Molecules 19, no. 10: 16447-16457.