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Molecules 2014, 19(11), 18558-18573; doi:10.3390/molecules191118558

Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells

1
Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, Krzywoustego 4, 44-100 Gliwice, Poland
2
Center for Translational Research and Molecular Biology of Cancer, Maria Sklodowska-Curie Memorial Cancer Center and Institute of Oncology, Gliwice Branch, Wybrzeze Armii Krajowej 15, 44-100 Gliwice, Poland
3
Pharmaceutical Research Institute, Rydygiera 8, 01-793 Warsaw, Poland
*
Author to whom correspondence should be addressed.
Received: 31 August 2014 / Revised: 5 November 2014 / Accepted: 7 November 2014 / Published: 13 November 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

The need to find new EGFR inhibitors for use in combination with radiotherapy in the treatment of solid tumors has drawn our attention to compounds derived from genistein, a natural isoflavonoid. The antiproliferative potential of synthetic genistein derivatives used alone or in combination with ionizing radiation was evaluated in cancer cell lines using clonogenic assay. EGFR phosphorylation was assessed with western blotting. Genistein derivatives inhibited clonogenic growth of HCT 116 cancer cells additively or synergistically when used in combination with ionizing radiation, and decreased EGFR activation. Our preclinical evaluation of genistein-derived EGFR inhibitors suggests that these compounds are much more potent sensitizers of cells to radiation than the parent isoflavonoid, genistein and indicate that these compounds may be useful in the treatment of colon cancer with radiation therapy. View Full-Text
Keywords: genistein glycoconjugates; epidermal growth factor receptor inhibition; radiotherapy; radiosensitization genistein glycoconjugates; epidermal growth factor receptor inhibition; radiotherapy; radiosensitization
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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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Gruca, A.; Krawczyk, Z.; Szeja, W.; Grynkiewicz, G.; Rusin, A. Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells. Molecules 2014, 19, 18558-18573.

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