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Vol. 26 No. 21 (2014): Vol 26 Issue 21

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Antitumor Activities and DNA-Binding Studies of Some Resveratrol Bioisosteres

https://doi.org/10.14233/ajchem.2014.17184
Xiaolin Tang
School of Chemistry & Pharmaceutical Science, Guangxi Normal University, Guilin 541004, Guangxi, P.R. China
Biqun Zou
Department of Chemistry, Guilin Normal College, Guangxi 541001, P.R. China
Xianghui Yi
Department of Chemistry, Guilin Normal College, Guangxi 541001, P.R. China
Yongzhi Liao
Department of Chemistry, Guilin Normal College, Guangxi 541001, P.R. China
Ye Zhang
Guangxi Academy of Fishery Sciences, Nanning 530021, P.R. China

Corresponding Author(s) : Yongzhi Liao

liao0777@163.com

Asian Journal of Chemistry, Vol. 26 No. 21 (2014): Vol 26 Issue 21

Abstract

Several bioisosteres of resveratrol (1-7) were designed and synthesized. The in vitro antitumour activities screening revealed that compound 1 exhibited better inhibition activities than the commercial anticancer drug 5-fluorouracil on MGC80-3 cell lines, with IC50 of 35.57 ± 1.49 μM and compound 2 showed higher cytotoxicity than 5-fluorouracil on A-375 cells, with IC50 of 44.09 ± 1.58 μM, while compound 3 displayed preferable inhibition than 5-fluorouracil on Hep G2 cells, with IC50 of 15.52 ± 0.86 μM, respectively. In addition, the binding properties of compounds 1-7 to DNA were investigated by fluorescence emission titration and the result shows that seven compounds have medium binding with DNA, with quenching constant values in the range of 102-103 L mol-1.

Keywords

Resveratrol Antitumor activity DNA-binding studies Bioisosterism
Tang, X., Zou, B., Yi, X., Liao, Y., & Zhang, Y. (2014). Antitumor Activities and DNA-Binding Studies of Some Resveratrol Bioisosteres. Asian Journal of Chemistry, 26(21), 7443–7445. https://doi.org/10.14233/ajchem.2014.17184
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