✦ LIBER ✦

A Simple Procedure for Preparation of N-Thiazolyl and N-Thiadiazolylcantharidinimides and Evaluation of Their Cytotoxicities against Human Hepatocellular Carcinoma Cells

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

Book ID: 102565589
Publisher: Elsevier Science
Year: 2000
Tongue: English
Weight: 85 KB
Volume: 28
Category: Article
ISSN: 0045-2068
DOI: 10.1006/bioo.2000.1178

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✦ Synopsis

We made an effort to prepare effective cantharidinimides by heating the reactants 1 and 2a-j to 200 degrees 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. Copyright 2000 Academic Press.

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