Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure–Activity Relationship

Abstract

Cancer, also known as malignant neoplasm, is a dreadful disease which involves abnormal cell growth having the potential to invade or spread to other parts of the body. Benzimidazole is an organic compound that is heterocyclic and aromatic in nature. It is a bicyclic compound formed by the fusion of the benzene and imidazole ring systems. It is an important pharmacophore and a privileged structure in medicinal chemistry. According to the World Health Organisation (2015 survey), one in six deaths is due to cancer around the globe, accounting for 8.8 million deaths of which 70% of the cases were from low- and middle-income countries. In the efforts to develop suitable anticancer drugs, medicinal chemists have focussed on benzimidazole derivatives. This review article covers the current development of benzimidazole-based anticancer agents along with the synthetic approaches and structure-activity relationships (SAR).

Three new mixed‐ligand copper(II) complexes containing glycyl‐l‐valine and N,N‐aromatic heterocyclic compounds: Synthesis, characterization, DNA interaction, cytotoxicity and antimicrobial activity

“…The higher antimicrobial activities of 1 and 2 compared with 3 may be attributed to the better biocompatibility of the benzimidazole‐like ligands . The antimicrobial activity of complex 1 was significantly greater than that of complex 2 , which may be mainly due to the relatively strong lipophilic property of HPBM compared with TBZ, having been verified by experiment.…”

“…Thus, studies of the differences can be favorable for thoroughly understanding the binding mechanism of copper complexes to DNA. So far, particular attention has been primarily focused on copper(II) complexes containing N,N‐aromatic heterocyclic compounds due to their high DNA binding ability and antiphlogistic, antibacterial and antitumor activities . Moreover, numerous copper complexes with various modified N,N‐aromatic heterocyclic compounds have been synthesized, and their DNA binding and cleavage activities have also been explored …”

Dinuclear copper(II) complex with a benzimidazole derivative: Crystal structure, theoretical calculations, and cytotoxic activity

“…candesartan and telmisartan) . Besides the pharmacological activities already mentioned, several studies demonstrated that benzimidazole derivatives also possess antitumoral and other relevant biological activities …”

Synthesis and In Vitro Urease Inhibition of Some Novel Benzimidazole‐based Hydrazones

“…Benzimidazoles are clearly known as significant chemical species with a wide range of biological activities including antioxidant , anticancer , antimicrobial , enzyme inhibition , and great potential. Benzimidazole and its derivatives have an important role in the field of medicine.…”