Xanthone is a novel and pharmacologically important oxygen containing hetrocyclic ring exhibiting variety of potent biological activities. This fused tricyclic ring is derived naturally from the plants of Bonnetiaceae and Clusiaceae family as well as synthesized by employing various synthetic protocols. Their wide range of reported therapeutic attributes include α-glucosidase inhibition, anti-cancer, anti-oxidant, anti-asthmatic, anti-convulsant, xanthine oxidase inhibition and anti-microbial. Among these attributes, anti-cancer and anti-oxidant potential are comprehensively studied as evidenced by number of research papers. Although, there is no marketed formulation containing xanthone derivatives except some herbal formulations, their medicinal properties can not be neglected at all. Promising activities revealed by these compounds chains their use and places them ahead as potential drug candidates for the future studies. Therefore, the present review article is entirely an assemblage of recent research work that has been done on xanthones and their analogs as therapeutic agents. This review article can be reasonably encouraging for those engaged in the area of developing efficient and effective, single therapeutic agent exhibiting a wide range of biological activities involving xanthone as crucial and central nucleus.