In Vitro and in Vivo Anticancer Activity of Copper Bis(thiosemicarbazone) Complexes
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https://figshare.com/articles/dataset/In_Vitro_and_in_Vivo_Anticancer_Activity_of_Copper_Bis_thiosemicarbazone_Complexes/2443246
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资源简介：
Neutral and cationic copper bis(thiosemicarbazone) complexes
bearing
methyl, phenyl, and hydrogen, on the diketo-backbone of the ligand
have been synthesized. All of them were characterized by spectroscopic
methods and in three cases by X-ray crystallography. In vitro cytotoxicity
studies revealed that they are cytotoxic unlike the corresponding
zinc complexes. Copper complexes Cu(GTSC) and Cu(GTSCHCl) derived
from glyoxal-bis(4-methyl-4-phenyl-3-thiosemicarbazone) (GTSCH2) are the most cytotoxic complexes against various human cancer
cell lines, with a potency similar to that of the anticancer drug
adriamycin and up to 1000 fold higher than that of the corresponding
zinc complex. Tritiated thymidine incorporation assay revealed that
Cu(GTSC) and Cu(GTSCHCl) inhibit DNA synthesis substantially. Cell
cycle analyses showed that Cu(GTSC) and Cu(GTSCHCl) induce apoptosis
in HCT116 cells. The Cu(GTSCHCl) complex caused distinct DNA cleavage
and Topo IIα inhibition unlike that for Cu(GTSC). In vivo administration
of Cu(GTSC) significantly inhibits tumor growth in HCT116 xenografts
in nude mice.
创建时间：
2016-02-19
