Oxindole has been shown to be a pharmacologically advantageous scaffold having many biological properties that are relevant to medicinal chemistry. The simplicity and widespread occurrence of this scaffold in plant-based alkaloids have further reinforced oxindole's merit in the domain of novel drug discovery. First extracted from Uncaria tomentosa, commonly the known as cat claw's plant which was found abundantly in the Amazon rainforest, molecules with the oxindole moiety have been shown to be common in a wide variety of compounds extracted from plant sources. The role of oxindole as a chemical scaffold for fabricating and designing biological drugs agents can be ascribed to its ability to be modified by a number of chemical groups to generate novel biological functions. This review is aimed at providing a description of the general chemistry based on existing corresponding structure-activity relationships (SARs) and compile all recent developmentary studies on oxindole-derived compounds as a successful pharmaceutical agent. A substantial group of oxindole derivatives are chiefly being tested as anticancer agents, however, a several oxindole derivatives have been shown to possesses antimicrobial, α-glucosidase inhibitory, antiviral, antileishmanial, antitubercular, antioxidative, tyrosinase inhibitory, PAK4 inhibitory, antirheumatoid arthritis and intraocular pressure reducing activities, to name a few. In this review we show the potential value of developing newer oxindole derivatives with an improved range of pharmacological implications as well as identifying drugs possessing oxindole core, that are showing and serving increased efficacy in clinical practice.