This review covers substantially the cytotoxic compounds isolated from endophytic fungi from terrestrial and mangrove plants during [2009][2010][2011][2012]. Endophytes living asymptomatically within plant tissues have been found in almost all plants studied to date. Many of the compounds reported here were originally isolated from plants, then from endophytic fungi, whereas some are exclusively isolated from endophytic fungi. The anticancer activities in this review are from the published cytotoxicity against specific cancer cell lines. Development of these natural compounds is based on their cytotoxic activity profiles, chemical structures, and potential structure-activity relationship deduced from the biochemical and cytotoxic studies.