This work initiates the original and updated literature review of the current state of research on the Saniculoideae subfamily, emphasizing the selected genera Saniculeae, namely Sanicula, Hacquetia, Astrantia, and Eryngium. Various parts of these plants, especially aerial parts and roots, have an immense range of medicinal uses in traditional medicine for a number of ailments. Phytochemical studies conducted on the Saniculeae species indicate that these plants synthesize metabolites belonging to diverse groups of compounds. These include triterpenoid saponins, flavonoids, phenolic acids, coumarins, volatile organic compounds, polyacetylenes, ecdysteroids, phytosterols, lignans, betaines, carotenoids, and anthraquinones. Some of the structures of these compounds are rare in the plant kingdom. The pharmacological potential of the Saniculeae species as antioxidant, anti-inflammatory, antimicrobial, antiviral, antiprotozoal, antitumor, antidiabetic, hypocholesterolemic, and neuroprotective agents has been explored in several studies. In addition, traditional medicinal uses have been discussed to provide a comprehensive picture of this subfamily. It is known that these plants have been used to treat dermatological diseases, respiratory issues, gastrointestinal problems, inflammations, wound healing, and cancers. As far as the author is aware, this is the first study conducted on this subfamily. Therefore, this review paper is the first to examine the little-known Saniculeae genera regarding their phytochemical and pharmacological characteristics. Studies showed that Saniculeae genera synthesize distinct secondary metabolites. Therefore, further research should be conducted on the exploration of these metabolites. The pharmacological investigation should also validate their potential efficacy in treating specific ailments and support their inclusion in modern healthcare practices.