Introduction: Coumarins are a group of plant-derived polyphenolic compounds. They belong to the benzopyrones family and possess a wide variety of cytoprotective and modulatory functions, which may be translated to therapeutic potentials for multiple diseases. Their physicochemical properties seem to define the extent of the biological activity.
Areas covered: In this review recent patent publications (2008 – 2011), describing coumarins and their derivatives, are analyzed. Synthesis, combinatorial techniques, biological evaluation in vitro/in vivo/ex vivo, e.g. antimitotic, immunomodulating, antiviral, anticancer and cytotoxic agents, as well as some new biological assays, are included. In addition to selected biological data, a wide range of pharmaceutical applications and pharmaceutical compositions are also summarized.
Expert opinion: Several natural and synthetic coumarins and derivatives with potent in vivo/in vitro biological responses appear to be promising anticancer activities. Their clinical evaluation will be critical to assess therapeutic utility. The compounds for which the mechanism of action is well defined can serve as lead compounds for the design of new more promising molecules.