Molecules | |
Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives | |
Zheng-Wei Li1  Wei Zhang2  Ya-Jun Li2  Fei Gao2  Yang-Feng Liu3  Li Wang4  Rui Xu4  | |
[1] Department of Anesthesia, The Affiliated Hospital of Xi'an Medical University, Xi'an 710077, China;Department of Neurology, The Affiliated Hospital of Xi'an Medical University, Xi'an 710077, China;Department of Neurology, The People’s Liberation Army No. 451 Hospital, Xi’an 710032, China;Department of Scientific Research, The Affiliated Hospital of Xi'an Medical University,Xi'an 710077, China; | |
关键词: phloretin derivatives; X-ray diffraction analysis; mechanism; anticancer activity; | |
DOI : 10.3390/molecules191016447 | |
来源: DOAJ |
【 摘 要 】
A 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.
【 授权许可】
Unknown