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

被引:153
作者
Ottanà, R
Carotti, S
Maccari, R
Landini, I
Chiricosta, G
Caciagli, B
Vigorita, MG
Mini, E
机构
[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
[2] Univ Florence, Dipartimento Farmacol Preclin & Clin, I-50139 Florence, Italy
关键词
antiproliferative activity; human colon cancer; thiazolidinones; cyclooxygenase;
D O I
10.1016/j.bmcl.2005.05.093
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3930 / 3933
页数:4
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