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

Authors
Lin, PY Shi, SJ Shu, HL Chen, HF Lin, CC Liu, PC Wang, LF
Citation
Py. Lin et al., A simple procedure for preparation of N-thiazolyl and N-thiadiazolylcantharidinimides and evaluation of their cytotoxicities against human hepatocellular carcinoma cells, BIOORG CHEM, 28(5), 2000, pp. 266-272
Citations number
10
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
BIOORGANIC CHEMISTRY
ISSN journal
00452068 → ACNP
Volume
28
Issue
5
Year of publication
2000
Pages
266 - 272
Database
ISI
SICI code
0045-2068(200010)28:5<266:ASPFPO>2.0.ZU;2-1
Abstract
We made an effort to prepare effective cantharidinimides by heating the rea ctants 1 and 2a-j to 200 degreesC 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. (C) 2000 Academic Press.