In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I

详细信息    查看全文

• 作者：Rosaria Ottanà ; Stefania Carotti ; Rosanna Maccari ; Ida Landini ; Giuseppa Chiricosta ; Barbara Caciagli ; Maria Gabriella Vigorita and Enrico Mini
• 关键词：Antiproliferative activity ; Human colon cancer ; Thiazolidinones ; Cyclooxygenase
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：2005
• 年：2005
• 卷：15
• 期：17
• 页码：3930-3933
• 全文大小：142 K

文摘

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.