The combination of traditional knowledge of medicinal plants with scientific rationale has yielded positive results in recent years. Bioactive compounds isolated from herbaceous plants have long been used as drugs that benefit human health, as well as providing useful compounds for drug development lead compound optimization. This chapter aims to provide a systematic overview of the structural types of Desmos secondary metabolites, along with their biological potential. Various chromatographic and spectroscopic methods have been utilized for isolating, purifying, and elucidating the structures of compounds from Desmos species. From 1982 to the present time, more than 200 metabolites have been isolated from members of this genus. Desmos spp. constituents include terpenoids, phytosterols, polyoxygenated cyclohexanes and cyclohexenes, oxepinones, fatty acids, with flavonoids, alkaloids, and miscellaneous phenols being the predominant compounds. The essential oils of Desmos species have also been investigated. Both crude plant extracts and isolated compounds from this genus have been evaluated for their biological activities. Desmos constituents have been found to exhibit cytotoxic, antimicrobial, antioxidative, anti-inflammatory, and aromatase and NFAT transcriptive inhibition effects.