Cynometra L. is a Fabaceae genus that is widely distributed throughout the tropics, consisting of tropical forest trees with ecological and economic importance since they are used as food and herbal medicines by the populations of their natural habitats. Our goal is to provide a review of the research data concerning the potential of this botanical genus as a source of herbal medicines and secondary metabolites that are useful for human health. To that end, scientific databases, including PubMed, Science Direct, ISI Web of Science, Scopus, and Google Scholar, were searched using the following terms: Cynometra, medicine, chemical, biological activity, toxicity, and “AND” as the Boolean connector. Eleven Cynometra species (9.7%) were reported to be used in traditional medicine to treat different ailments. A total of 185 secondary metabolites of various chemical classes, mainly flavonoids and terpenoids, were identified in eight Cynometra species (7.1%). Vitexin was the only flavonoid identified as bioactive in the sequence of bioguided studies on this botanical genus. Ten species (8.8%) were submitted to in vitro and in vivo biological activity assays. The main evaluated activities were in vitro antioxidant, antimicrobial, cytotoxic, and in vivo anti-inflammatory activities, but no human clinical trials or safety data about this genus were found. Cynometra cauliflora and Cynometra ramiflora were the most studied species. The present work confirms the use of Cynometra species as a source of medicinal plants. However, more experimental studies must be conducted to better understand this botanical genus’s usefulness as a source of raw materials for pharmaceutical use.