ABSTRACT A series of hydroxyxanthones has been synthesized and screened for their anti-AChE activity. This led to the discovery of new AChE inhibitors with the highest inhibitory activity of IC50 69.45±0.23 M. A neurotoxicity evaluation revealed that hydroxyxanthones represented another class of compound that was non-toxic to the neuroblastoma cells at IC50 higher than 94 M.