The genus Malvastrum, from the family Malvaceae, is a small genus of twenty four species, distributed worldwide. Some of the species have a long and rich history of ethnobotanical and traditional medicinal uses. Few reports of systematic scientific studies can be found in the literature which highlight the rich chemical profile and pharmacological properties of the genus. This is the first ever attempt to compile the available literature and provide a critical overview for future studies on the genus. For this purpose, several databases, such as PubMed, Scifinder, Elsevier, Google Scholar, and others were utilized. Literature records the presence of bioactive metabolites in the genus, effective against dysentery, gastrointestinal distress, fever, enteritis, hepatitis, cough, sore throat, arthritis, and diabetes. Seventy four biologically active secondary metabolites have been identified from different species of Malvastrum, including four pure isolates. Furthermore, this report also documents their potential properties. This article may prove as a milestone for new researchers, eager to work on Malvastrum species and perform further in-depth studies on this genus.