Medicinal plants of the genus Walsura (family Meliaceae) are native to tropical zones of a number of Asian countries, and have been used in systems of folk medicine. Several original research articles on Walsura species are available, but an overview highlighting the phytochemical and biological aspects of the compounds isolated to date is so far absent. Since the 1970s, phytochemical investigations on the genus Walsura have been undertaken, and more than 220 compounds from ten species have been identified. Natural products from Walsura species that have received the most attention are limonoids (114 compounds) and triterpenoids (72 compounds). Walsura limonoids have been characterized structurally as having diverse skeletons and more than 100 such compounds are new to the literature, while dammaranes, tirucallanes, and apotirucallanes are the main triterpenoid types from this genus. Other Walsura constituents comprise sesquiterpenoids, flavonoids, sterols, lignans, xanthones, and anthraquinones. Walsura species constituents have also been studied in natural product drug discovery screening programs. Many in vitro biological and some in vivo pharmacological investigations have been carried out on Walsura species isolated compounds. Walsura components display properties such as cancer cell cytotoxicity, antimicrobial, antidiabetes, anti-inflammatory, antioxidant, antifeedant, antifertility, ichthyotoxic, and neuroprotection activities.