A Simple Procedure for Preparation of N-Thiazolyl and N-Thiadiazolylcantharidinimides and Evaluation of Their Cytotoxicities against Human Hepatocellular Carcinoma Cells.
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.
Pen-Yuan
L
School of Pharmacy, School of Medicine, Department of Biochemistry, Taipei Medical University, 250 Wu-Shing Street, Taipei, Taiwan
Sheng-Jie
S
Hsien-Liang
S
Hsue-Fen
C
Chiung-Chang
L
Pong-Chun
L
Leng-Fang
W