Review Article

Synthesis of Diflunisal Thiazolidinones as Anticancer Agents

Author(s):

Sevil Şenkardeş, Özlem B. Özakpınar, Derya Özsavcı, Azize Şener, Özge Çevik and Ş. Güniz Küçükgüzel   Pages 1266 - 1274 ( 9 )

Abstract:

A series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2',4'-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl- 3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 μM. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH- 3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC₅₀ value of 5.2 μM against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.

Keywords:

Annexin-V, apoptosis, diflunisal, K-562 cancer cell line, 4-Thiazolidinone.

Affiliation:

, , , , , Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey.

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