Background. Genus Miliusa (family Annonaceae), widely distributed in mainland Asia and Australia to New Guinea, has been employed in both traditional herbal uses and pharmacological medicines. Original research articles related to this genus are now available, but supportive reviews highlighting phytochemical and pharmacological aspects are now insufficient. Objective. This account is an overview of most of the compounds isolated from this genus, along with their pharmacological evaluations. Conclusion. A vast amount of data showed that genus Miliusa contained various classes of secondary metabolites. Herein, more than two hundred constituents were isolated, comprising alkaloids, geranylated homogentisic acids, flavonoids, lignans, neolignans, terpenoids, acetogenins, styryls, lactones, phenolics, amides, alcohols, and furfural derivatives. Novel miliusanes and bicyclic lactones have been remarkable characteristics of Miliusa plants. Essential oils from these plants were also detected, with a high amount of β-caryophyllene. Numerous in vitro biological researches on, for example, anticancer, antifungal, antimycobacterial, anti-inflammation, and cardiac activity, especially in terms of cytotoxicity, using either isolated compounds or plant extracts, implied that Miliusa phytochemical components now set out to have a key role in pharmacological development. M. smithiae ethyl acetate extract and its flavonoid ayanin (75) inhibited the growth of MCF-7 cell line comparable with positive control ellipticine. (+)-Miliusol (72) stimulated in vivo anticancer experiment against HCT116 xenograft mouse tumor following the p21-dependent induction of cellular senescence mechanism.