<p>For over four decades, the Inuleae tribe has been the focus of extensive research, initially centered on the morphological traits of its species to develop a comprehensive taxonomic classification. In recent years, molecular studies have further refined this classification, offering deeper insights into the phylogenetic relationships within the tribe. Currently, the Inuleae tribe comprises more than 600 species, organized into approximately 60 genera, distributed worldwide with a high degree of endemism. Investigations of the biochemical composition of these species have unveiled remarkable chemodiversity, particularly in their terpene and terpenoid profiles. These compounds have shown potent activities across a range of biological targets, including the neutralization of free radicals, antimicrobial effects, and anticancer properties. Additionally, they have shown significant anti-inflammatory effects, inhibited key enzymes related to other diseases, such as acetylcholinesterase and tyrosinase, and demonstrated strong efficacy against insect pests. This review provides a comprehensive analysis of the chemical diversity of terpenoids through characterization and typification, while also covering botanical aspects and bioactivity.</p> Graphical abstract <p></p>