Pseudotsuga is a crucial genus of timber trees in the Pinaceae family, comprising approximately 18 species that are predominantly found in western North America and East Asia. Over the past several decades, scholarly attention has primarily focused on the phytochemical study of Pseudotsuga menziesii, revealing a diverse range of compounds, including monoterpenes, sesquiterpenes, and flavonoids. Notably, recent advancements have also identified rare triterpene-monoterpene and triterpene-diterpene adducts, as well as triterpenoid dimers, from the Pseudotsuga genus. In this review, we comprehensively cover studies on Pseudotsuga species, comprising isolated compounds and their potential biological activities. The present review demonstrates that Pseudotsuga species exhibit a wide spectrum of pharmacological activities, largely attributed to the activities of terpenoids, flavonoids, and phenolics. These discoveries not only enrich our understanding of the chemical diversity of the Pseudotsuga genus but also highlight its potential in pharmaceutical and therapeutic applications.