Natural products have always been important resources either as therapeutic agents or as lead compounds for the production of pharmaceutical compounds. Osthole, 7-methoxy-8-(3-methyl-2-butenyl) coumarin, an ingredient of a Traditional Chinese Medicine(TCM), has received considerable attention recently because of its significant and diverse pharmacological activities, including anticancer, antisteoporotic, and antiproliferative, which make it a very promising natural lead compound for new drug discovery. The present work summarizes the related biological information on osthole and its analogues and proposes the possibility of its development as a promising lead compound for drug discovery.