A series of substituted pyrimidinyl (thio)semicarbazide derivatives were
designed and synthesized. The antitumor results showed that the activity of thiosemicarbazide
compounds (series II) was generally higher than that of the corresponding
semicarbazide derivatives (series I). Among them, IIk displayed higher cytotoxicity
against HL-60, BGC-823 and Bel-7402 than that of adriamycin and exhibited broad in
vitro cytotoxicity against 13 human tumor cell lines. Meanwhile, the cytotoxic selectivity and anti-multidrug resistance
were evaluated, and IIk exhibited selective cytotoxicity against cancer cells in comparison to human normal cells and had
significant anti-multidrug resistance capability. The bioassay results showed that IIk showed great promise as a potent
lead compound for further antitumor discovery.
Keywords: Synthesis, (thio)semicarbazide, antitumor activity, multidrug resistance.
Rights & PermissionsPrintExport