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Benzofuran formed by the condensation of furan nucleus with benzene ring are not common in the nature. However numerous synthetic benzofuran derivatives found to possess wide range of biological activities. Benzofuran was initially aimed at the research work on the isolation of biologically active products possessing furan and benzofuran ring system. The structures of such compounds range from simple to highly complex molecules 5-methoxybenzofuran. A great variety of both synthetic and naturally occurring molecules that include benzo [b] furan motif in their structure have been reported to show diverse biological activities and other special features, which provide them with potential applications in the fields of biomedicine and material sciences. These derivatives exhibit significant activity including antifungal, antiprotozoal, antitubercular, antiinflammatory, anticonvulsant, anticancer, antiHIV, analgesic, antiparasitic, antihyperlipidemic, antioxidant, antidiabetic, antihypertensive, antiplasmodial, Alzheimer's, vasodilating and hypotensive, arrhythmic, anti-histaminic, antidepressant, antitumor activities.