A simple procedure for preparation of N-thiazolyl and N-thiadiazolylcantharidinimides and evaluation of their cytotoxicities against human hepatocellular carcinoma cells

Lin Pen-Yuan, Shi Sheng-Jie, Shu Hsien-Liang, Chen Hsue-Fen, Lin Chiung-Chang, Liu Pong-Chun, Leng-Fang Wang

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32 Citations (Scopus)


We made an effort to prepare effective cantharidinimides by heating the reactants 1 and 2a-j to 200°C with toluene and triethylamine to provide 10 N-thiazolyl- and N-thiadiazolylcantharidinimides 3a-j in high yields of 48-91%. All of the synthetic compounds were tested for their capability to suppress growth of the human hepatocellular carcinoma cell lines, SK-Hep-1 and Hep 3B. The results showed that compound 3f was the most potent, and it was more cytotoxic than cantharidin.

Original languageEnglish
Pages (from-to)266-272
Number of pages7
JournalBioorganic Chemistry
Issue number5
Publication statusPublished - 2000



  • Cantharidin
  • Cytotoxicity
  • Human hepatocellular carcinoma cell
  • N-thiadiazolylcantharidinimide
  • N-thiazolylcantharidinimide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery

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