Isatin (1 H -indole-2,3-dione) is a heterocyclic compound, involved in many pharmacological activities. Significant amount of data has been publis hed about its pharmaceutical importance; therefore, a comprehensive overview of recent de velopments is required. This revi ew will provide a brief account on the recent advancements and future perspectives in the pharmacol ogical aspects of isatin and its derivatives reported in last six years. Besides ma ny other pharmacological activities, isatin and its derivatives have been found to show promising results against various cancer cell lines and a large range of pathogenic microbes. Isatin is a versatile precursor for many biological active molecules. Most of the work done reported in literature is about in vitro studies and only few examples are in vivo studies in rats. Therefore, a more systematic and targ eted scientific research is required to use these therapeutically potent molecules as drugs.