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Molecules 2014, 19(10), 16447-16457; doi:10.3390/molecules191016447

Synthesis, Crystal Structure, and Biological Evaluation of a Series of Phloretin Derivatives

1,†,* , 2,†, 3,†, 1, 3, 4 and 3,*
1
Department of Scientific Research, The Affiliated Hospital of Xi'an Medical University, Xi'an 710077, China
2
Department of Anesthesia, The Affiliated Hospital of Xi'an Medical University, Xi'an 710077, China
3
Department of Neurology, The Affiliated Hospital of Xi'an Medical University, Xi'an 710077, China
4
Department of Neurology, The People’s Liberation Army No. 451 Hospital, Xi’an 710032, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 12 August 2014 / Revised: 10 September 2014 / Accepted: 23 September 2014 / Published: 13 October 2014
(This article belongs to the Section Organic Synthesis)
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Abstract

A one-step synthesis of phloretin derivatives 211 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 911 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
Keywords: phloretin derivatives; X-ray diffraction analysis; mechanism; anticancer activity phloretin derivatives; X-ray diffraction analysis; mechanism; anticancer activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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.

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