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Tang X.,Guangxi Normal University | Zou B.,Guilin Normal CollegeGuangxi | Yi X.,Guilin Normal CollegeGuangxi | Liao Y.,Guilin Normal CollegeGuangxi | Zhang Y.,Guangxi Academy of Fishery science
Asian Journal of Chemistry | Year: 2014

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. © 2014, Chemical Publishing Co. All rights reserved. Source


Fang Y.,Hunan UniversityHunan | Yi X.,Guilin Normal CollegeGuangxi | Qin W.,Guilin Normal CollegeGuangxi | Zhang Y.,Guilin Normal CollegeGuangxi | Liao Y.,Guangxi Academy of Fishery science
Asian Journal of Chemistry | Year: 2014

A series of 2-oxo-quinoline-3-Schiff-base derivatives (4a1-4n2) have been designed and synthesized as new antitumor agents. in vitro Antitumor activities were evaluated against four cancer cell lines including MGC80-3, BEL-7404, A549 and NCI-H460. Compounds 4a1, 4a2, 4c2, 4d1, 4d2 and 4l2 exhibited better inhibition activities than commercial antitumor drug 5-fluorouracil (5-fluorouracil, IC50 = 44 ±0.54 μM) on NCI-H460, with IC50 of 35.52 ± 0.86, 16.22 ± 0.71, 11.62 ± 0.52, 5.16 ± 0.37, 7.62 ± 0.46 and 7.66 ± 0.65 μM, respectively. © 2014, Chemical Publishing Co. All rights reserved. Source

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