engleski

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

3-Hydroxypyridin-4-ones are a well known class of heterocyclic compounds extensively studied due to 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. 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] In the continuation of our work novel lipophilic adamantyl derivatives of meta N- aryl substituted 3-hydroxy-2- methylpyridin-4-ones were prepared with the aim of evaluating their in vitro antitumor properties on the panel of cancer cell lines. The compounds were synthesized starting from corresponding pyridinones, which are prepared first in an autoclave, and subsequently acylated with adamantan-1-ylacetic acid. Further structure-activity relationship study (SAR) of such and similar pyridinone derivatives as potential anticancer agents is now in progress. Antitumor properties of novel compounds started to elucidate the key elements, primarily the nature and position of the substituent on the aryl part on the adamantyl pyridinones, needed for their high antiproliferative activity. Keywords: adamantan-1-ylacetic acid, antitumor activity, 3- hydroxypyridin-4-ones, [1] M.A. Santos, S. Chaves, Future Med. Chem. 7 (2015) 383-410. [2] V. Petrović Peroković, Ž. Car, T. Opačak- Bernardi, I. Martin-Kleiner, M. Kralj, S. Tomić, Mol. Div. 21 (2017) 881-891.

adamantan-1-ylacetic acid, antitumor activity, 3-hydroxypyridin-4-ones,

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