Chorisia (syn. Ceiba) is a genus of approximately 20 species of large, perennial, and deciduous trees within the plant family Bombacaceae, with common geographical distribution throughout the subtropical and tropical regions, especially South America. Besides their well-known ornamental and economic value, members of the genus Chorisia have found applications as medicinal plant species thanks to their assortments of bioactive phytoconstituents. To date, about 273 structurally varied metabolites have been described from different plant parts of Chorisia plants using various chromatographic and spectroscopic techniques, which mainly included flavonoids, anthocyanins, phenolic acids, quinones, terpenoids, and steroids, among others. Moreover, several organic solvent extracts and purified metabolites from Chorisia plants have been tested for their biological potential, such as anti-inflammatory, analgesic, antipyretic, antioxidant, hepatoprotective, antiobesity, cytotoxic, antidiabetic, hypolipidemic, antiulcerogenic, and antimicrobial properties. In of view of that, the current work provides an overview on different phytochemicals reported from the genus Chorisia as well as various biological and toxicological studies conducted so far on these plants, along with future research perspectives that might help expand their phytotherapeutic applications.