Farag Basant, Zaki Magdi E A, Elsayed Doaa A, Gomha Sobhi M
Department of Chemistry, Faculty of Science, Zagazig University Zagazig 44519 Egypt
Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU) Riyadh 11623 Saudi Arabia
RSC Adv. 2025 Jun 3;15(23):18593-18647. doi: 10.1039/d5ra01077b. eCollection 2025 May 29.
A six-membered benzene ring is fused with a five-membered imidazole ring at positions four and five, generating benzimidazole, the benzo derivative of imidazole and a bicyclic aromatic chemical compound. Benzimidazole is a significant pharmacophore in a variety of physiologically active heterocyclic compounds due to its distinctive characteristics and structural framework. Because benzimidazole is both aromatic and heterocyclic, it interacts with a range of biological targets metal ion interactions, π-π stacking, and hydrogen bonding. Its broad range of medicinal chemistry applications, such as anti-inflammatory, antiviral, antifungal, and anticancer therapies, is based on these interactions. Its significance in the development of potentially novel therapeutic pharmaceuticals is highlighted by the fact that its structural flexibility permits the synthesis of derivatives with targeted bioactivity. Derivatives of benzimidazole have garnered significant research interest as potential anticancer medications. These heterocyclic compounds exhibit a wide range of biological activities, such as DNA interaction, enzyme inhibition, and modulation of cellular pathways crucial to cancer development. Thus, to optimize their therapeutic potential, recent studies have focused on evaluating the structure-activity relationships (SAR) of benzimidazole derivatives. The main topics of this review are the current developments in the synthesis, anticancer activity, and SAR studies of benzimidazole derivatives, which will shed light on the increasing role they play in cancer therapies.
一个六元苯环在4位和5位与一个五元咪唑环稠合，生成苯并咪唑，它是咪唑的苯并衍生物，也是一种双环芳香化合物。由于其独特的特性和结构框架，苯并咪唑是多种生理活性杂环化合物中的重要药效基团。由于苯并咪唑既是芳香族又是杂环化合物，它与一系列生物靶点发生相互作用，包括金属离子相互作用、π-π堆积和氢键作用。其广泛的药物化学应用，如抗炎、抗病毒、抗真菌和抗癌治疗，都基于这些相互作用。其结构灵活性允许合成具有靶向生物活性的衍生物，这一事实凸显了其在开发潜在新型治疗药物方面的重要性。苯并咪唑衍生物作为潜在的抗癌药物已引起了大量研究兴趣。这些杂环化合物表现出广泛的生物活性，如DNA相互作用、酶抑制以及对癌症发展至关重要的细胞途径的调节。因此，为了优化其治疗潜力，最近的研究集中在评估苯并咪唑衍生物的构效关系（SAR）。本综述的主要主题是苯并咪唑衍生物在合成、抗癌活性和SAR研究方面的当前进展，这将揭示它们在癌症治疗中日益重要的作用。
