Benzocoumarins are coumarins with a phenyl group bonded to 3,4-, 5,6-, 6,7-, or 7,8-positions. Over the past
years, significant efforts have been made not only to isolate the novel structural analogs of benzocoumarins with
prominent bioactivities but also to design new synthetic methods to synthesize benzocoumarins with better or novel
biological properties. The aim of this review is to provide the readers with an overview of the research progress of
benzocoumarins from 1953 to May 2014, covering its isolation, synthesis, and biological activities.