With the development of exploration for disease-related proteins or receptors, more and more novel structural lead compounds are required to designed and synthesized. The benzimidazole is an effective structural unit in which the benzene ring is fused at the 4 and 5 positions of the imidazole ring and wildly used in drug design. Here, we introduce some recent progress of research for anti-tumor agents which was target to various target proteins such as DNA topoisomerase, angiogenesis, serine/threonine protein kinase, and tyrosine protein kinase. These anti-tumor agents are all introduced benzimidazole as the structure unit. Further docking study showed that the benzimidazole group was not only act as a skeleton to expand the structure of molecule but also as an excellent ligand unit to form hydrogen bond or π–π conjugation and hydrophobic interaction with target proteins or receptors. We expect that introducing benzimidazole in the chemical structure could be a reasonable and priority strategy in novel anti-tumor agents' design.

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以苯并咪唑为结构单元的抗肿瘤药物研究进展

随着疾病相关蛋白或受体探索的发展，需要设计和合成越来越多的新型结构先导化合物。苯并咪唑是一种有效的结构单元，其中苯环稠合在咪唑环的4和5位，广泛用于药物设计。本文介绍了针对DNA拓扑异构酶、血管生成、丝氨酸/苏氨酸蛋白激酶、酪氨酸蛋白激酶等多种靶蛋白的抗肿瘤药物的研究进展。这些抗肿瘤药物均以苯并咪唑为结构单元引入。进一步的对接研究表明，苯并咪唑基团不仅可以作为骨架扩展分子结构，而且可以作为优良的配体单元与靶蛋白或受体形成氢键或π-π共轭和疏水相互作用。我们预计在化学结构中引入苯并咪唑可能是新型抗肿瘤药物设计中合理且优先的策略。