Malvaceae sensu lato is a family containing about 245 genera and 4,465 species mainly distributed across tropical and subtropical regions worldwide. Species of this family usually contain alkaloids with anti-inflammatory, antinociceptive, antiparasitic, antimicrobial and anticancer properties due to its secondary metabolites. In this context, this review aims to checklist the alkaloids isolated from Malvaceae sensu lato species, evaluating their chemical profile and pharmacological potential, providing a broad and concise overview of these secondary metabolites. The results were collected from scientific databases such as Web of Science, Scifinder, Pubmed, ScienceDirect and Google Scholar, using the keywords “Alkaloids” and “Malvaceae”. Several pharmacological/ biological activities are reported in literature for the most varied alkaloid nuclei, such as: vasorelaxation of the mesentery of rats (cryptolepinone), antitrypanosomal activity (waltherione) and anti-inflammatory and bronchodilator activity (vasicine), which highlights a succession of activities related to this class of secondary metabolites. Presented data report the importance of the Malvaceae sensu lato family, demonstrating the biological relevance of its alkaloids, in order to contribute to scientific knowledge and the development of new drugs.