In Vitro and in Vivo Anticancer Activity of Copper Bis(thiosemicarbazone) Complexes

摘要: Neutral and cationic copper bis(thiosemicarbazone) complexes bearing methyl, phenyl, hydrogen, on the diketo-backbone of ligand have been synthesized. All them were characterized by spectroscopic methods in three cases X-ray crystallography. In vitro cytotoxicity studies revealed that they are cytotoxic unlike corresponding zinc complexes. Copper Cu(GTSC) Cu(GTSCHCl) derived from glyoxal-bis(4-methyl-4-phenyl-3-thiosemicarbazone) (GTSCH(2)) most against various human cancer cell lines, with a potency similar to anticancer drug adriamycin up 1000 fold higher than complex. Tritiated thymidine incorporation assay inhibit DNA synthesis substantially. Cell cycle analyses showed induce apoptosis HCT116 cells. The complex caused distinct cleavage Topo II alpha inhibition for Cu(GTSC). vivo administration significantly inhibits tumor growth xenografts nude mice.