<p>Conferone is one of the most abundant sesquiterpene coumarins isolated from the <i>Ferula</i> and <i>Heptaptera</i> genera. In addition to three exported medicinal products, the genus <i>Ferula</i> is also used in traditional medicine to treat cough, asthma, toothache, stomach problems, and constipation. Conferone, as one of 31 sesquiterpene coumarins identified from the roots of <i>Ferula</i> species, has shown various medicinal activities such as anti-inflammatory, cytotoxic, P-glycoprotein (P-gp) inhibitor, anticancer, and anti-leishmanial. Despite recent studies on the anticancer activity of conferone, most of the related literature is usually scattered in different publications, which limits the possibility of further research on this secondary metabolite. This comprehensive review, collected conferone data from 1972 to August 2023 using major databases such as PubMed, Science Direct, Google Scholar, etc. Although there are not many published papers on this sesquiterpene coumarin. However, this review article aims to promote more research on conferone by summarizing the available literature on sources, extraction methods, isolation, identification, and determination of the structure to investigate the biological activities and the relationship of its structure with the reported activities. Therefore, in the present work, while reviewing the in vitro and in silico studies conducted on conferone, in the end, a critical evaluation will be presented to highlight the strengths and limitations along with solutions to solve them.</p> Graphical abstract <p></p>