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Novel para N-aryl substituted 3-hydroxypyridin-4- ones and their adamantyl derivatives

3-Hydroxypyridin-4-ones are nowadays widely investigated for their broad spectrum of biological activities (antibacterial, antidiabetes, antiprotozoal, antineurodegenerative and anticancer).[1] In our previous work we investigated several para N-aryl substituted 3- hydroxy-2-methylpyridin-4-ones as well as their ester adamantyl derivatives for their in vitro antitumor properties on several cancer cell lines. All tested compounds showed antiproliferative activity ranging from moderate to strong on all inspected cell lines with lipophilic adamantane containing derivatives being active at low micromolar IC50 concentrations.[2] Further structure-activity relationship study (SAR) of such and similar pyridinone derivatives as potential anticancer agents is now in progress. In this work, for the purpose of that study, novel para N-aryl substituted 3-hydroxy-2-methylpyridin- 4-ones containing different substituents on the same position of the aryl part as well as their adamantyl derivatives were prepared (Fig. 1). All compounds were prepared with the aim of evaluating their in vitro antitumor properties on the panel of cancer cell lines. Antitumor properties of novel compounds started to elucidate the key elements, primarily the nature of the substituent on the aryl part on the adamantyl pyridinones, needed for their high antiproliferative activity.

3-hydroxypiridin-4-one, antiproliferative activity

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