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

Research output: Contribution to journalArticlepeer-review

Abstract

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
Volume28
Issue number5
DOIs
Publication statusPublished - 2000

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Biology
  • Biochemistry
  • Organic Chemistry

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