Synthesis and antiproliferative evaluation of some iron chelators as polyamine transporter targeting agents

Abstract

A series of kojic acid derivatives based on monoamines, diamines, and triamines have been synthesized in good yield and purity. A spermidine (spd) rescue experiment was applied against MCF-7 cells to evaluate the polyamine transporter selectivity, and in vitro antiproliferative effects were determined against Hela and DU-145 cell lines. Overall, 5b showed the best selectivity for the polyamine transporter and antiproliferative effects. Therefore, the in-silico metabolism profile and ADMET properties of the title compounds were calculated by the PreADMET server. Additionally, physicochemical properties of ligands were predicted by using the Molinspiration online property calculation server.