, CO, and various oxidants. This review also explores the structure-activity relationships of isoindolin-1-one derivatives in diverse therapeutic areas. Specific functional groups and substituents have been shown to enhance anticancer, antiviral, antipsychotic, antimicrobial, cardiovascular, anti-inflammatory, and antidiabetic activities. Modifications including lipophilic, electron-withdrawing, polar, and heterocyclic moieties have significantly improved biological efficacy, target specificity, and pharmacokinetics. The integration of these structural variations underscores the scaffold's versatility and its potential in drug discovery. This review aims to provide a consolidated foundation for future research on isoindolin-1-one based therapeutics and their strategic synthesis.