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Breast and gynecological cancers are major health concerns due to their increasing incidence rates, and in some cases, their low survival probability. In recent years, multiple compounds of natural origin have been analyzed as alternative treatments for this disease. For instance, Acetogenins are plant secondary metabolites from the Annonaceae family, and its potential anticancer activity has been reported against a wide range of cancer cells both in vitro and in vivo. Several studies have demonstrated promising results of Acetogenins' antitumor capacity, given their selective activity of cellular inhibition at low concentrations. This review outlines the origin, structure, and antineoplastic activities in vitro and in vivo of Acetogenins from Annonaceae against breast cancer and gynecological cancers reported to date. Here, we also provide a systematic summary of the activity and possible mechanisms of action of Acetogenins against these types of cancer and provide references for developing future therapies based on Acetogenins and nanotechnologies. [Display omitted] • Acetogenins show anticancer effects in gynecological and breast cancers. • Compounds like bullatacin, annonacin, and bullacin B show potent anticancer activity. • The acetogenins interrupt the respiratory chain by inhibiting mitochondrial complex I. • The Bis-THF acetogenins demonstrate stronger anticancer activities. • The use of nanosystems to administer acetogenins enhances drug efficacy. [ABSTRACT FROM AUTHOR]