Isatin is a heterocyclic nitrogen compound that has attracted much interest in recent years due to its diverse biological and pharmacological activities. It can be used in many medical and biological applications, such as antidiabetic, antibiotic, and anticancer agents. The isatin molecule can also be prepared from different substrates by various methods, such as the methods of Sandmeyer, Stolle, Gassman, Meanwell and Hewawasam and others. On the other hand, the isatin molecule can undergo various chemical reactions, such as oxidation, Friedel-Crafts reaction, ring expansion, aldol condensation, and alkylation reactions. As a result of these reactions, several biologically useful biomolecules are formed, including 2-oxindoles, tryptanthrin, indirubins and others. Therefore, the aim of this review was to provide an overview of the synthetic methods of the isatin molecule and its derivatives and to examine the various chemical reactions it undergoes. In addition, a list of some of the recently documented biological activities of isatin derivatives was compiled, such as antidiabetic, antibacterial, anticancer, and other properties.