Synthesis and Antitumor Activity of Novel N-Benzoyl-N'-substituted Pyrimidinyl (Thio)semicarbazide Derivatives

Author(s): Gaopeng Song, Jianzuo Li, Hao Tian, Yasheng Li, Dekun Hu, Ying Li, Zining Cui

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 4 , 2016

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Graphical Abstract:


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.

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Article Details

Year: 2016
Page: [329 - 334]
Pages: 6
DOI: 10.2174/1570180812666151003002644
Price: $65

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