<p>The Amaryllidaceae family encompasses numerous species characterized by a distinct group of alkaloids. Amaryllidaceae exhibit a wide distribution in all Brazilian biomes, with Cerrado hosting 29 species spanning five genera (<i>Crinum</i>, <i>Griffinia</i>, <i>Hippeastrum</i>, <i>Nothoscordum</i>, and <i>Zephyranthes</i>). An integrative review was conducted to assess the extent of available information documented in the literature concerning the chemical composition or biological activity of these 29 species. Among the examined species, <i>Crinum americanum</i> L., <i>Crinum jagus</i> (J.Thomps) Dandy, <i>Hippeastrum glaucescens</i> (Mart.) Herb.<i>,</i> and <i>Hippeastrum puniceum</i> (Lam.) Kuntze emerged as the most extensively studied regarding chemical composition and biological activity. Conversely, no comprehensive reports on the chemistry and biological activity of <i>Nothoscordum</i> species were identified. Remarkably, data deficiency persists for 70% of the assessed species, underscoring the underexplored nature of Amaryllidaceae occurring in the Cerrado biome, notwithstanding their pharmacological and ornamental potential. Given the precarious state of the Cerrado vegetation, which ranks among the most threatened in South America, it is imperative to investigate these plants and explore sustainable ways for harnessing their inherent potential.</p> Graphical abstract <p></p>