Gliomas, originating from glial cells, are prevalent and aggressive brain tumors with high recurrence rates and poor prognosis. Despite advancements in surgical, radiation, and chemotherapeutic treatments, the survival rates remain low. Current standard therapies, such as Temozolomide, have limitations due to cytotoxicity, restricted effectiveness, and severe side effects. So, the development of safer anti-glioma agents is the need of the hour. Bioactive compounds of plant origin, either natural or synthetic, have potential implications due to them actively attacking different targets with a wide range of bioactivities, including anti-glioma activities. In this review, for the first time, there is an overall overview of 51 small molecules of plant origin and seven of their synthetic derivatives, represented as anti-glioma agents in the past decades. The goal of the present review is to provide a summary to comprehend the anti-glioma effects of these compounds in addition to providing a reference for preclinical research into novel anti-glioma agents for future clinical application.