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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