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The employment of phytomolecules to treat cancer has become widespread in recent decades. Boswellic acids (BAs) are pentacyclic triterpenoids obtained from Boswellia oleo-gum resins. BAs are the primary active constituents of Boswellia resins and exhibit potent anticancer activity against numerous cancer cell lines. Consequently, they have garnered considerable attention as prominent anti-cancer agents. However, the pharmacokinetic characteristics of BAs, such as their low bioavailability and poor water solubility, pose significant barriers that limit their medicinal use. The aim of this review is to provide a thorough overview of the anticancer effects of BAs, along with their physiochemical parameters, pharmacokinetic profile, and structure–activity relationship (SAR). Furthermore, computational studies conducted on BAs to improve their therapeutic efficacy, relevant clinical studies evaluating BAs, the associated challenges, and future prospects have also been discussed. A systematic review of the literature was conducted to identify the effects of BAs in various cancers. The following databases were searched: PubMed, Web of Science, and Scopus, for prospective studies published between 2012 and 2025. Although BAs exhibit significant therapeutic potential, their clinical utility is limited by their pharmacokinetic profile. Focused studies on improved isolation techniques, the development of synthetic derivatives, and hybrid molecules are required to address these challenges. In addition, advancements in nanodrug delivery systems and computational studies are vital to overcome these barriers. Collectively, these strategies could prove helpful in establishing BAs as privileged scaffolds for developing anticancer drugs.
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