Benzimidazole scaffolds have potent anticancer activity due to their structure similarity to nucleoside. In addition, benzimidazoles could function as hydrogen donors or acceptors and bind to different drug targets that participate in cancer progression. The literature had many anticancer agents containing benzimidazole cores that gained much interest. Provoked by our endless interest in benzimidazoles as anticancer agents, we summarized the successful trials of the benzimidazole scaffolds in this concern. Moreover, we discuss the substantial opportunities in cancer treatment using benzimidazole-based drugs that may direct medicinal chemists for a compelling future design of more active chemotherapeutic agents with potential clinical applications. The uniqueness of this work lies in the highlighted benzimidazole scaffold hybridization with different molecules and benzimidazole-metal complexes, detailed mechanisms of action, and the IC₅₀ of the developed compounds determined by different laboratories after 2015.

苯并咪唑支架由于其结构与核苷相似而具有有效的抗癌活性。此外，苯并咪唑可以充当氢供体或受体，并与参与癌症进展的不同药物靶标结合。文献中有许多含有苯并咪唑核心的抗癌药物引起了人们的广泛兴趣。出于我们对苯并咪唑作为抗癌药物的无尽兴趣，我们总结了苯并咪唑支架在这方面的成功试验。此外，我们讨论了使用苯并咪唑类药物治疗癌症的巨大机会，这些机会可能会指导药物化学家在未来设计出具有潜在临床应用的更活性的化疗药物。这项工作的独特之处在于突出了苯并咪唑支架与不同分子和苯并咪唑-金属配合物的杂交、详细的作用机制以及2015年后不同实验室测定的所开发化合物的IC ₅₀ 。