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This is exemplified by the fact that several isatin\u2010based anticancer agents, such as semaxanib, sunitinib, nintedanib, and hesperadin, are already in use or under clinical trials for the treatment of diverse kinds of cancers. Isatin\u2010based hybrids could be obtained by incorporating other anticancer pharmacophores into the isatin skeleton and they have the potential to overcome drug resistance with reduced side effects. Thus, isatin\u2010based hybrids may provide attractive scaffolds for the development of novel anticancer agents. This review covers the recent advances of isatin\u2010based hybrids with anticancer activity, covering articles published between 2001 and 2019. The anticancer activities of these molecules and the structure\u2013activity relationships are also discussed. 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