Department of Pharmaceutical Chemistry, School of Pharmaceutical Education & Research, Hamdard University, Hamdard Nagar, New Delhi-110062, India
Department of Pharmaceutical Chemistry, Indo Soviet Friendship College of Pharmacy, Ghal Kalan, Ferozpur G.T. Road MOGA-142001, Punjab, India
Curr Med Chem. 2020;27(35):5970-6014. doi: 10.2174/0929867326666190808122929.
This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.
这篇综述详细介绍了导致癌症的因素，并介绍了合成苯并咪唑衍生物作为抗癌药物的设计策略。2017 年美国化学学会的《癌症事实与数据》最近对癌症治疗的调查显示，抗癌工作取得了进展。世界各地的研究人员，无论是在发达国家还是发展中国家，都在不断努力解决这一严重问题。由于与天然存在的含氮碱基即嘌呤相似，苯并咪唑及其衍生物表现出广泛的生物活性。该综述讨论了通过不同机制表现出抗癌特性的苯并咪唑衍生物，即嵌入剂、烷化剂、拓扑异构酶、DHFR 酶和微管蛋白抑制剂。苯并咪唑衍生物通过不同的机制发挥作用，早期和最近的研究文章中报道的取代基是合成靶向苯并咪唑衍生物作为抗癌药物的前提。该综述重点通过图中呈现的 SAR 轻松比较了发挥效力和选择性所必需的取代基。这将进一步提供更好的前景或满足开发新型苯并咪唑衍生物作为抗癌药物所面临的挑战。
