Coumarins, a natural class of compounds, firstly isolated from Tonka beans, are found in various medicinal herbs. This class of compounds has been reported of remarkable biological and pharmacological applications, including antimicrobial, anticoagulants, anti-inflammatory as well as cancer. Additionally, coumarins have revealed significant inhibition of different human cancers viz bladder cancer, lung cancer, prostate cancer, ovarian cancer, colon cancer, breast cancer, gastric cancer, leukemia, pancreatic cancer, etc. Therefore, the compilation of medicinal research progress of natural coumarin and its derivatives will be beneficial for scientists and researchers worldwide. The literature review of medicinal research progress of natural coumarin and its derivatives was collected from various databases, including PubMed, Web of Science and Science Direct from the year 1942 to date. The presented data on medicinal research progress of natural coumarin and its derivatives provides a detailed review which could serve as a platform for future research. The data presented the medicinal and biological activities of coumarin and its derivatives like antimicrobial, anticoagulant, anti-inflammatory and anticancer in particular. This could be utilized for future formulation and development of drugs and references based on coumarin and its derivatives.