New 8-heterocyclic xanthine derivatives as antiproliferative agents: Synthesis and biological evaluation

Abstract

This research focuses on the synthesis, characterization, and evaluation of the anti-cancer activity of novel 8-aryl substituted 1,3-diethylxanthine derivatives. The anti-proliferative activities of all the compounds were assessed using an MTT assay on four human cancer cell lines: breast cancer MCF7, human lung cancer A549, human brain cancers LN229, and U87. One of the derivatives of 1,3-diethylxanthine with a thiazole structure displayed strong anti-proliferative activity. 1,3-Diethyl-8-(thiazol-4-yl)-3,7-dihydro-1H-purine-2,6-dione (5) exhibited the strongest activity against A549, MCF7, LN229, and U87 cell lines, with IC50 values of 16.70, 78.06, 22.07, and 25.07 μM, respectively. Furthermore, the scratch assay was conducted to evaluate the effect of compound 5 on the inhibition of cell migration in A549 cells. The consistent results demonstrate that compound 5 exhibits potent anticancer activity, which could be further investigated to enhance its biological potential.