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The recent emergence of anticancer activity of thiourea derivatives have inspired the medicinal chemist to design and synthesize new thiourea derivatives. These thiourea based anticancer chemotherapeutics inhibit cancer propagation by acting as inhibitors of topoisomerase, protein tyrosine kinase, somatostatin agonists, sirtuins, and carbonic anhydrase (CA). This review summarizes the recent developments on the thiourea based anticancer chemotherapeutics.