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Isoindole derivatives constitute an important class of biologically active heterocyclic compounds and continue to attract considerable attention due to their diverse pharmacological profile such as, antimicrobial, anthelmintic, insecticidal, cyclooxygenase isoenzyme (COX-2) and thrombin inhibition with special emphasis on anticancer activity. This review highlights anticancer properties of isoindole derivatives and its related structures and hoping that it would further help in generation of new concepts towards rational design and development of more potent and less toxic anticancer agents.