Synthesis of novel unsymmetrical alkyl-aryl-selenides: β-carbonyl-selenides derivatives and anticancer evaluation

As a new kind of unsymmetrical alkyl-aryl-selenides, a series of novel β-carbonyl-selenides derivatives were synthesized with high regioselectivity and substrates tolerance. Total six series and forty-four compounds were generated. The in vitro antiproliferative activities were evaluated on U251-MG, U87-MG, MDA-MB-231, HCT116 and SW620 cells lines. Structure and antiproliferative relationship were discussed. Among them, (±)-N, N′-(1,2-phenylene)-bis-(2-((3-oxobutan-2-yl)selanyl) benzamide) ( 5t ) has significant antiproliferative activity and potential value as anticancer agent with IC 50 values < 2.63 µM, while the IC 50 values of Ebselen > 86.36 µM in test tumor cells.