Synthesis and biological evaluation of bidentate 3-hydroxypyridin-4-ones iron chelating agents

L Saghaie, H Sadeghi-aliabadi, M Kafiri


A series of 3-hydroxypyridin-4-one derivatives (HPOs) were synthesized and their partition coefficient values (Kpart) were determined. The cytotoxic effects of these iron chelators against Hela cancer cells were also evaluated. The IC50 of HPOs was determined using MTT assay. Among these ligands, compound 4e (Kpart=5.02) with an IC50 of 30 µM and 4f (Kpart=0.1) with an IC50 of 700 µM showed the lowest and highest IC50's, respectively. In conclusion, the introduction of a more hydrophobic functional group (such as butyl in compound 4e) on the nitrogen of pyridinone ring resulted in higher cytotoxic activity of ligands.

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