Exploration of benzimidazoles as potential microtubule modulators: An insight in the synthetic and therapeutic evolution

• Published in: Journal of molecular structure 2022-04, Vol.1253, p.132251, Article 132251
• Main Authors: Laxmikeshav, Kritika, Himaja, Ambati, Shankaraiah, Nagula
• Format: Article
• Language: English
• Subjects: Anticancer activity; Benzimidazole; Microtubule inhibitors; Molecular hybridization; Structure-activity relationship
• ISSN: 0022-2860; 1872-8014
• DOI: 10.1016/j.molstruc.2021.132251

The dynamic microtubules are one of the most fruitful targets for cancer chemotherapy. The outcomes of various studies depict that the benzimidazole framework is a fundamental moiety in various synthetic analogues, signifying a myriad scope of therapeutic activities. These scaffolds have also established their place as prospective tubulin polymerisation inhibitors in the medicinal chemistry arena. In this regard, the current review demonstrates a comprehensive report on the design and synthetic strategies engaged in developing various benzimidazole-bearing heterocyclic molecules as promising cytotoxic agents acting as tubulin polymerisation modulators. The detailed assessment of antiproliferative activities with reference drugs allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesised benzimidazole hybrids. •This review provides an extensive overview of the synthesis and anticancer activity of benzimidazole derivatives developed in the last decade.•The synthetic protocols and representative active molecules are depicted along with GI50 and/or IC50 values against different cancer cell lines.•The structural activity relationship study and binding mode with tubulin has also been highlighted. [Display omitted]