review · Molecular Diversity
Benzimidazole scaffolds show potent anticancer activity because their chemical structure is similar to nucleosides. Their ability to act as both hydrogen donors and acceptors allows them to bind to a variety of biological targets involved in cancer development and progression. A substantial body of research published after 2015 demonstrates the successful application of benzimidazole cores in developing experimental anticancer compounds. These designs include hybridising benzimidazole scaffolds with other functional molecules as well as creating benzimidazole-metal complexes. By detailing the mechanisms of action and reported inhibitory concentration values from multiple laboratories, this synthesis of findings maps current progress in the field. These insights provide strategic pathways to guide medicinal chemists in rational drug design, aiming to produce more active chemotherapeutic candidates suited for prospective clinical use.
Cancer therapies require new chemical compounds capable of targeting tumours through diverse mechanisms. Benzimidazoles offer a versatile molecular framework that mimics natural biological components, making them effective building blocks for novel drugs. Clarifying how these compounds interact with cancer targets helps scientists design more potent treatments, potentially improving efficacy and expanding options for future clinical therapies.
This work supports early-stage drug discovery by offering design strategies for medicinal chemists and pharmaceutical developers working on novel chemotherapies. The highlighted molecular hybrids and metal complexes provide starting points for preclinical optimisation. Because the underlying data focus on laboratory-measured inhibitory concentrations and mechanisms of action, these compounds remain at an early exploratory research stage, requiring substantial preclinical validation and formal testing before any clinical translation or market use can occur.
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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 IC<sub>50</sub> of the developed compounds determined by different laboratories after 2015.
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DOI: 10.1007/s11030-024-10907-8
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