Synthesis and Biological Evaluation of 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives as Potential Cytotoxic Agents

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  • Shi Yao-Jie
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University
  • Song Xue-Jiao
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University
  • Li Xiao
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University
  • Ye Ting-Hong
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University
  • Xiong Ying
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University
  • Yu Luo-Ting
    State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University

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A series of new 3-amino-5-sulfanyl-1,2,4-triazole and 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives have been synthesized and their cytotoxicities were evaluated on a panel of human cancer cell lines (BxPC-3, H1975, SKOV-3, A875, HCT116, etc.). The best one (compound 5m) exhibited activities with IC50 values ranging from 0.04 to 23.6 µM against nine human cancer cell lines. Further biological evaluation indicated that DNA replication was blocked by treatment with compound 5m in HCT116 cells.

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