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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of Diflunisal Thiazolidinones as Anticancer Agents
Volume: 16 Issue: 10
Author(s): Sevil Şenkardeş, Özlem B. Özakpınar, Derya Özsavcı, Azize Şener, Özge Çevik and Ş. Güniz Küçükgüzel
Affiliation:
Keywords: Annexin-V, apoptosis, diflunisal, K-562 cancer cell line, 4-Thiazolidinone.
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.
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Şenkardeş Sevil, Özakpınar B. Özlem, Özsavcı Derya, Şener Azize, Çevik Özge and Küçükgüzel Güniz Ş., Synthesis of Diflunisal Thiazolidinones as Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (10) . https://dx.doi.org/10.2174/1871520615666150831125337
DOI https://dx.doi.org/10.2174/1871520615666150831125337 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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