A number of species of genus Grewia have been used as medicinal agents to treat several diseases. This review based on 45 literary sources discusses the current knowledge of traditional uses, chemistry, biological effects, and toxicity of different species of this genus. Triterpenoids, steroids, glycosides, flavones, lignans, phenolics, alkaloids, lactones, anthocyanins, flavones, and organic acids have been isolated from various species of this genus. The extracts and preparations from the various plants, which are expectantly safe, exhibited various biological effects, e.g. anti-oxidant, anti-bacterial, hepatoprotective, anti-inflammatory, anti-emetic, anti-malarial, analgesic, and anti-pyretic activities.