Synthesis of Diflunisal Thiazolidinones as Anticancer Agents

Author(s): Sevil Şenkardeş , Özlem B. Özakpınar , Derya Özsavcı , Azize Şener , Özge Çevik , Ş. Güniz Küçükgüzel .

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 10 , 2016

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Graphical 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.

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Article Details

Year: 2016
Page: [1266 - 1274]
Pages: 9
DOI: 10.2174/1871520615666150831125337
Price: $58

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