Bis-coumarins have caused great interests in the recent years. These compounds exhibit diverse biological activities which are ascribed to their ability to exert noncovalent interactions with the various active sites in organisms. Some of them such as dicoumarolum and dicoumarol were approved for therapeutic purposes in clinical practice. Encouraged by the above facts, numerous biscoumarin derivatives have been synthesized and screened for their biological activities, and many of them showed promising potency. This review is focused on the biological potential of bis-coumarin derivatives with particular mention of those exhibiting antibacterial, anticoagulant, antiinflammatory, antiviral, anti-parasite and antitumor activities, and their structure-activity relationships are also discussed.