Natural Epidithiodiketopiperazine Alkaloids As Potential Anticancer Agents: Recent Mechanisms of Action, Structural Modification, and Synthetic Strategies

•The sources, classification, structural characteristics, and anticancer potential of natural epidithiodiketopiperazine (ETP) alkaloids are summarized (1970–2023).•The mechanisms of action of several ETP alkaloids with anticancer activity are reviewed (2009–2023).•The structural modifications and synthetic strategies for several ETP alkaloids with anticancer activity are listed (2009–2023).•This review highlights the tremendous potential of ETP alkaloids and their derivatives as lead compounds for further anticancer drug development.