Patil Shital M, Nikalje Piyush, Gavande Navnath, Asgaonkar Kalyani D, Rathod Vaishnavi
Department of Chemistry, AISSMS College of Pharmacy, Kennedy Road, Pune-01, India.
Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA.
Curr Top Med Chem. 2025;25(4):350-377. doi: 10.2174/0115680266343336241021080438.
Cancer is a leading cause of death worldwide, driving the urgent need for new and effective treatments. Benzimidazole and pyrazole derivatives have gained attention for their potential as anticancer agents due to their diverse biological activities. The development of resistance in cancer cells, toxicity concerns, and inconsistent efficacy across different types of cancer are a few of the challenges. To overcome these challenges, optimisation of these nuclei using the structure-activity relationships is necessary.
This review aimed to examine various benzimidazole, pyrazole, and their hybrid derivatives by focusing on their structure-activity relationships (SAR) as anticancer agents. Results of the most potent and least potent benzimidazole, pyrazole compounds, and their hybrid derivatives published by researchers were compiled.
The findings of different researchers working on benzimidazole and pyrazole nuclei were reviewed and analysed for different targets and cell lines. Moreover, substitutions on different positions of pyrazole, benzimidazole, and their hybrid were summarised to derive an optimised pharmacophore.
Based on our analysis of existing studies, we anticipate that this review will guide researchers in creating potent pyrazole, benzimidazole, and hybrid derivatives crucial for combating cancer effectively.
Structure-Activity Relationship (SAR) studies can help in developing pyrazolebenzimidazole hybrids that are more powerful and selective in targeting specific aspects of cancer.
癌症是全球主要的死亡原因之一，这促使人们迫切需要新的有效治疗方法。苯并咪唑和吡唑衍生物因其多样的生物活性而作为抗癌剂的潜力受到关注。癌细胞耐药性的产生、毒性问题以及不同类型癌症中疗效不一致等都是面临的一些挑战。为克服这些挑战，有必要利用构效关系对这些核心结构进行优化。
本综述旨在通过关注苯并咪唑、吡唑及其杂化衍生物作为抗癌剂的构效关系（SAR）来研究各种此类化合物。整理了研究人员发表的最具活性和活性最低的苯并咪唑、吡唑化合物及其杂化衍生物的结果。
对研究苯并咪唑和吡唑核心结构的不同研究人员针对不同靶点和细胞系的研究结果进行了综述和分析。此外，总结了吡唑、苯并咪唑及其杂化物不同位置上的取代情况，以推导优化的药效团。
基于我们对现有研究的分析，预计本综述将指导研究人员开发出对有效对抗癌症至关重要的强效吡唑、苯并咪唑和杂化衍生物。
构效关系（SAR）研究有助于开发在靶向癌症特定方面更有效且更具选择性的吡唑苯并咪唑杂化物。
