Advances of Benzimidazole Derivatives as Anticancer Agents: Bench to Bedside

Kashif Haider, M. Shahar Yar
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引用次数: 2

Abstract

Benzimidazole is one of the privileged nitrogen-containing scaffolds known for its versatile diversified role in insecticides, pesticides, dyes, pigments and pharmaceuticals. Due to its electron-rich environment, structural features and binding potency of various therapeutic targets, benzimidazole derivatives exhibit a broad spectrum of biological activity that majorly includes antimicrobial, antifungal, analgesics, anti-diabetic and anticancer agents. Several benzimidazole scaffolds bearing drugs are clinically approved; they are used for various indications. For example, Bilastine, Lerisetron, Maribavir and Nocodazole are the most widely used benzimidazole-based marketed drugs available as an antihistamine, antiviral and antimitotic agent, respectively. Another example is the recently approved anticancer drug Binimetinib and Selumetinib, which are indicated for BRAF mutated melanoma and plexiform neurofibromas. Not only this, many benzimidazole-based anticancer drugs are in late phases of clinical development. Due to the vast therapeutic potential of benzimidazole scaffold in cancer research, medicinal chemists have gained a lot of attraction to explore it more and develop novel, highly effective and target-specific benzimidazole-based potential anticancer drugs.
苯并咪唑类抗癌药物的研究进展:从实验到临床
苯并咪唑是一种特殊的含氮支架,在杀虫剂、农药、染料、颜料和药物中发挥着多种多样的作用。苯并咪唑衍生物由于其富含电子的环境、结构特点和与多种治疗靶点的结合能力,具有广泛的生物活性,主要包括抗菌、抗真菌、镇痛、抗糖尿病和抗癌等。几种苯并咪唑支架药物已获临床批准;它们用于各种适应症。例如,比拉斯汀、莱司琼、马里巴韦和诺可达唑是市面上使用最广泛的以苯并咪唑为基础的药物,分别作为抗组胺药、抗病毒药物和抗有丝分裂剂。另一个例子是最近批准的抗癌药物比尼美替尼和塞鲁美替尼,它们适用于BRAF突变的黑色素瘤和丛状神经纤维瘤。不仅如此,许多以苯并咪唑为基础的抗癌药物正处于临床开发的后期阶段。由于苯并咪唑支架在癌症研究中的巨大治疗潜力,药物化学家对其进行更多的探索,开发新型、高效、靶向的苯并咪唑类潜在抗癌药物受到了极大的关注。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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