In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I
The characterization of two cyclooxygenase isoforms (COX), the rate-limiting enzyme for the synthesis of prostaglandins (PGs) from arachidonic acid, has allowed the development of COX-2 selective inhibitors as non-steroidal anti-inflammatory drugs (NSAIDs) with significant gastric tolerability. Howe...
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Published in | Bioorganic & medicinal chemistry letters Vol. 15; no. 17; pp. 3930 - 3933 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
01.09.2005
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | The characterization of two cyclooxygenase isoforms (COX), the rate-limiting enzyme for the synthesis of prostaglandins (PGs) from arachidonic acid, has allowed the development of COX-2 selective inhibitors as non-steroidal anti-inflammatory drugs (NSAIDs) with significant gastric tolerability. However, PGs are also important in cancer pathogenesis. Thus, there is an increasing interest in studying COX-2 inhibitors as potential drugs aimed at the prevention and treatment of cancer, especially colorectal cancer. The purpose of this study was to determine the inhibitory effects of some representative 4-thiazolidinones, already widely investigated as potential NSAIDs, on the growth of five human colon carcinoma cell lines with a different COX-2 expression, and to correlate them with COX-2 inhibitory properties. Our results preliminarily revealed that 2-phenylimino derivative
3 and 2,4-thiazolidindione
4 were the most active compounds. In particular,
3 mainly inhibited the HT29 cell line characterized by a high COX-2 expression, whereas
4 showed antiproliferative properties on all tested cell lines, suggesting molecular targets other than COX-2 inhibition. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2005.05.093 |