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

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

  • Bioorg Med Chem Lett. 2005 Sep 1;15(17):3930-3. doi: 10.1016/j.bmcl.2005.05.093.
Rosaria Ottanà 1 Stefania Carotti Rosanna Maccari Ida Landini Giuseppa Chiricosta Barbara Caciagli Maria Gabriella Vigorita Enrico Mini
Affiliations

Affiliation

  • 1 Dipartimento Farmaco-chimico, Università di Messina,Viale SS. Annunziata, 98168 Messina, Italy.
Abstract

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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