Heteropterys is the largest genus in the botanical family Malpighiaceae that comprises more than 140 species. In the last years there has been an increasing interest on Heteropterys species because of the promising results of the pharmacological studies that explored Heteropterys species for first time. The objective of this review is to provide an overview of the active constituents isolated from Heteropterys genus, highlighting the aspects reported on the diversity of the biological activities tested during the past years. For this purpose, we reviewed the scientific literature available for the total number of species that belong to Heteropterys in specialized databases. Our findings showed that the properties on CNS (anxiolytic, antidepressant, improving learning and memory), the antioxidant effects and the protective activities of reproductive male organs are the most important biological activities reported for species of Heteropterys. Flavonoids are the chemicals most conspicuous, following by aliphatic nitro compounds and hydroxycinnamic acids identified in Heteropterys. This review pretend to be helpful for phytochemists and pharmacologist in the proposal of Heteropterys as potential source of metabolites that could be used to drug prototypes to many and diverse pathological or physiological situations.