This article aims to review the scientific data on phytochemical and pharmacological studies of Artocarpus collected from Malaysia as well as to highlight their usage as ethnomedicine worldwide. About 55 Artocarpus species are distributed worldwide and 32 of the Artocarpus species can be found in Malaysia. Artocarpus species are well known worldwide for their edible fruits such as Artocarpus heterophyllus (jackfruit), Artocarpus integer (chempedak), and Artocarpus communis (breadfruit). Aside from its edible fruits, the timber is valued for light constructions, crates, large canoes, and boats. The literature for this review was searched using the term ‘Artocarpus’, ‘Artocarpus Malaysia’, ‘Artocarpus extracts’, ‘Artocarpus traditional medicine’ and ‘Artocarpus ethnomedicine’ from published books and scientific journals via various engines such as The Web of Science, PubMed, Science Direct, Scopus, Research Gate, and Google Scholar. The references cited from the retrieved articles were also scanned and cross-checked. All published studies on phytochemical and pharmacological activities of Malaysia’s Artocarpus species up to January 2021 were included in this review. Articles on phytochemical studies of Malaysia’s Artocarpus revealed the isolation of flavonoids as the major constituents. Research on pharmacological activities of the isolated phytochemicals showed that these compounds exhibited significant disease-linked-enzyme (tyrosinase, cholinesterase, glucosidase) inhibitors as well as antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities. The ethnomedicinal data gathered are useful to understand and prioritize Artocarpus species that can contribute to potent phytochemicals and possibly new drug leads. This review also provides valuable information for the future development of isolated compounds from Artocarpus species.