Int. J. Mol. Sci. 2013, 14(5), 9424-9439; doi:10.3390/ijms14059424
Article

Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents

1,†email, 1,†email, 2email, 1,* email, 3email and 1,* email
Received: 31 January 2013; in revised form: 12 April 2013 / Accepted: 15 April 2013 / Published: 29 April 2013
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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.
Abstract: Several rhein-phosphonate derivatives (5ac) were synthesized and evaluated for in vitro cytotoxicity against HepG-2, CNE, Spca-2, Hela and Hct-116 cell lines. Some compounds showed relatively high cytotoxicity. Especially compounds 5b exhibited the strongest cytotoxicity against HepG-2 and Spca-2 cells (IC50 was 8.82 and 9.01 µM), respectively. All the synthesized compounds exhibited low cytotoxicity against HUVEC cells. Further experiments proved that 5b could disturb the cell cycle in HepG-2 cells and induce apoptosis. In addition, the binding properties of a model conjugate 5b to DNA were investigated by methods (UV-Vis, fluorescence, CD spectroscopy). Results indicated that 5b showed moderate ability to interact ct-DNA.
Keywords: rhein; phosphonate; synthesis; cytotoxicity; apoptosis; DNA binding
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MDPI and ACS Style

Ye, M.-Y.; Yao, G.-Y.; Wei, J.-C.; Pan, Y.-M.; Liao, Z.-X.; Wang, H.-S. Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents. Int. J. Mol. Sci. 2013, 14, 9424-9439.

AMA Style

Ye M-Y, Yao G-Y, Wei J-C, Pan Y-M, Liao Z-X, Wang H-S. Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents. International Journal of Molecular Sciences. 2013; 14(5):9424-9439.

Chicago/Turabian Style

Ye, Man-Yi; Yao, Gui-Yang; Wei, Jing-Chen; Pan, Ying-Ming; Liao, Zhi-Xin; Wang, Heng-Shan. 2013. "Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents." Int. J. Mol. Sci. 14, no. 5: 9424-9439.


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