Lee Yeuan Ting, Tan Yi Jer, Oon Chern Ein
Institute for Research in Molecular Medicine (INFORMM), Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
Acta Pharm Sin B. 2023 Feb;13(2):478-497. doi: 10.1016/j.apsb.2022.09.010. Epub 2022 Sep 21.
Cancer is the second leading cause of mortality globally which remains a continuing threat to human health today. Drug insensitivity and resistance are critical hurdles in cancer treatment; therefore, the development of new entities targeting malignant cells is considered a high priority. Targeted therapy is the cornerstone of precision medicine. The synthesis of benzimidazole has garnered the attention of medicinal chemists and biologists due to its remarkable medicinal and pharmacological properties. Benzimidazole has a heterocyclic pharmacophore, which is an essential scaffold in drug and pharmaceutical development. Multiple studies have demonstrated the bioactivities of benzimidazole and its derivatives as potential anticancer therapeutics, either through targeting specific molecules or non-gene-specific strategies. This review provides an update on the mechanism of actions of various benzimidazole derivatives and the structure‒activity relationship from conventional anticancer to precision healthcare and from bench to clinics.
癌症是全球第二大致死原因，如今仍然对人类健康构成持续威胁。药物不敏感性和耐药性是癌症治疗中的关键障碍；因此，开发针对恶性细胞的新实体被视为高度优先事项。靶向治疗是精准医学的基石。苯并咪唑的合成因其显著的药用和药理特性而引起了药物化学家与生物学家的关注。苯并咪唑具有杂环药效基团，这是药物和制药开发中的重要支架。多项研究已证明苯并咪唑及其衍生物作为潜在抗癌治疗药物的生物活性，其作用机制要么是通过靶向特定分子，要么是非基因特异性策略。本综述提供了各种苯并咪唑衍生物作用机制的最新情况，以及从传统抗癌到精准医疗保健、从实验室到临床的构效关系。
