Synthesis and biological evaluation of 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential cytotoxic agents.

نویسندگان

  • Yao-Jie Shi
  • Xue-Jiao Song
  • Xiao Li
  • Ting-Hong Ye
  • Ying Xiong
  • Luo-Ting Yu
چکیده

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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عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 61 11  شماره 

صفحات  -

تاریخ انتشار 2013