Acetogenins are a unique class of bioactive phytochemicals found only in the family of Annonaceae plants. Structurally, they consist of a terminal g-lactone ring bearing a hydrocarbon chain with various hydroxyls, acetoxyls, ketones, epoxides, tetrahydrofuran (THF) and tetrahydropyran (THP) rings together with double and triple bonds located within the chain. According to the searching of “acetogenin” as a keyword from SciFinder database 2014, it revealed that a great number of publications about acetogenin derivatives derived from the family have been reported. They displayed a broad biological property spectrum covering anticancer, antimalarial, antifungal, antituberculosis, and antioxidant effects together with the inhibition of electron transport chain in mitochondrial complex I and brine shrimp lethality activity. Therefore, this present article aimed to review the newly isolated acetogenins and their pharmacological activities published during the period from 2005 to 2014. From the systematically tabulated data, it is notable that most of them showed significantly biological activities towards selected human cancerous cell lines. Moreover, asimitrin (62), 4-hydroxytrilobin (68), and squamostanins A-D (78-81) demonstrated higher potency than adriamycin drug which is used to date. It is indicated that they should be considered as one of bioactive compounds for further development to be effective cancer drugs which are very useful in medicine.