Coumarin derivatives: an updated patent review (2015-2016)

Abstract

Introduction: Coumarins belong to the benzopyrone family. They are naturally plant-derived or synthetically obtained substances, presenting a wide variety of biological activities, offering an extented therapeutic profile. Their structural characteristics correlated to physicochemical properties define their pleiotropic biological responses.

Areas covered in this review: Recent patent publications (2015-2016), describing coumarins and their derivatives are analyzed. Synthesis, biological evaluations in vitro /in vivo e.g. antiviral, anticancer, cytotoxic, antioxidant, anti-inflammmatory protocols are included. Furthermore, several pharmaceutical applications and pharmaceutical compositions are also described. Expert opinion: Several synthetic coumarins, hybrids and derivatives (azoles, sulfonyl, furazan, pyrazole etc) have been found to possess promising anticancer, antitumor anti-proliferative 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 potent molecules.

Keywords: Anti-Alzheimer; MAO inhibitors; anticancer; antimicrobial; antioxidant; antiviral; coumarin; cytotoxicity.