Benzimidazole based derivatives as anticancer agents: Structure activity relationship analysis for various targets

Abstract

Benzimidazole, the benzo derivative of imidazole, is a class of bicyclic aromatic organic compound consisting of six‐membered benzene ring fused to five‐membered imidazole at 4‐ and 5‐positions of the imidazole ring. It is a vital pharmacophore of many biologically active heterocyclic compounds with a variety of pharmacological activities. Over the time, benzimidazole and its derivatives have evolved as vibrant heterocyclic systems due to their potency in a wide range of bioactive compounds like analgesics, antifungals, anti‐inflammatory, antihypertensives, proton pump inhibitors, anti‐HIV, antiviral, and so on. Multi‐drug resistance in cancer that led to the failure of many chemotherapeutic drugs is a major concern. Various approaches are being developed to overcome this problem. One of them is target based drug discovery, which is an effective method to develop a novel anticancer drug. To develop newer drugs, previously reported work needs to be studied. Keeping this in mind, last 5 years literature on benzimidazole used as anticancer agents has been reviewed and summarized in the paper herein. This review article along with the target of cancer also deal with structure activity relationship of various compounds having benzimidazole ring.

New Potential Agents for Malignant Melanoma Treatment—Most Recent Studies 2020–2022

“…Benzimidazole is a six-membered benzene ring fused to an imidazole ring at the 4-position and 5-position of the imidazole ring. Its derivatives exert antitumor activity mainly by inhibiting tubulin polymerization, kinase, and topoisomerase inhibitors, apoptosis inducers, and telomerase inhibitors [ 36 ]. Benzimidazole derivatives with anti-melanoma activity are presented in Figure 3 .…”

Novel 1,2,5-Trisubstituted Benzimidazoles Potentiate Apoptosis by Mitochondrial Dysfunction in Panel of Cancer Cells

“…The literature survey revealed that the benzimidazole derivatives have been extensively investigated as potential anticancer agents, and these benzimidazole derivatives exhibit anticancer effects through different mechanisms of action such as intercalating mode of action (DNA binding), nonintercalating mode of action (topoisomerases inhibition), DNA alkylation (DNA cleavage), acting on enzyme antimetabolites [DihydrofolateReductase (DHFR) inhibition], sirtuin inhibition (SIrt1 and SIrt2 inhibition), acting on structural proteins (tubulin protein inhibition), and protein kinase inhibition. − …”

Synthesis, characterization, biological evaluation, and computational study of benzimidazole hybrid thiosemicarbazide derivatives

“…[ 31 ] Because of their importance in a variety of industries, including nutrition, cosmetics, and medicines, many scientists have studied their chemistry and have produced a wide range of benzimidazole derivatives over the last few decade. [ 32 ] Benzimidazole derivatives have been found to be effective in numerous biochemical and pharmacological activities [ 33 ] such as anti‐HIV, [ 34 ] antihistaminic, [ 35 ] antioxidant, [ 36 ] antiulcer, [ 37 ] antimalarial, [ 38 ] analgesic, [ 39 ] anti‐tubercular, [ 40 ] antiinflammatory, [ 41 ] antihypertensive, [ 42 ] antimicrobial, [ 43 ] antiprotozoal, [ 44 ] antihelmintic, [ 45 ] anticancer, [ 46 ] antidiabetic, [ 47 ] antihypertensive, [ 48 ] DNA binding, [ 49 ] and antifungal [ 50 ] activities.…”