Benzimidazole and its derivatives as cancer therapeutics: The potential role from traditional to precision medicine

Lee, Yeuan Ting; Tan, Yi; Oon, Chern Ein

doi:10.1016/j.apsb.2022.09.010

Cited by 99 publications

(32 citation statements)

References 187 publications

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“…Additionally, many marketed drugs contain benzimidazole building block as XIII, Abemaciclib, XIV, Dovitinib, XV, Binimetinib, and XVI, Selumetinib (Fig. 4) [18]. Compound XVII showed promising anticancer activity with IC50 ranging from 2.2 µM to 11.9 µM against MCF7, MDA-MB231 and A549 cell lines comparable to 5-FU as a reference drug with IC50 ranging from 1.16 µM to 7.12 µM.…”

Section: XIImentioning

confidence: 99%

New Oxadiazole/ Benzimidazole Hybrids: Design, Synthesis, and Molecular Docking Studies.

Hagar

Abbas

Sayed

et al. 2023

Journal of advanced Biomedical and Pharmaceutical Sciences

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Five new oxadiazole/benzimidazole hybrids were designed and synthesized as EGFR inhibitors. The structure of the new compounds was confirmed with 1 H NMR and 13 C NMR as well as elemental analyses. Molecular docking studies were done to investigate their binding mode in ATP binding site of EGFR. The synthesized hybrids exhibited good binding in EGFR binding site. The thiol tautomers got better docking scores than thione ones. The docking scores of hybrids ranged from -7.4 kcal/mol to -8.7 kcal/mol which were comparable to that of the co-crystalized ligand Erlotinib (score = -9.7 kcal/mol). In silico physicochemical and pharmacokinetic properties prediction of them indicated that they have drug like properties.

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Section: XIImentioning

confidence: 99%

New Oxadiazole/ Benzimidazole Hybrids: Design, Synthesis, and Molecular Docking Studies.

Hagar

Abbas

Sayed

et al. 2023

Journal of advanced Biomedical and Pharmaceutical Sciences

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“…Benzimidazole cores are extensively occurring in a wide range of natural and pharmacologically active compounds. These molecules have been widely perceived in fields of biological and medicinal chemistry [99–103] owing to their recognition as bactericides, [104a] anti‐carcinogens, [104b–d] peptic ulcer activities, [104e–f] factor Xa (FXa) inhibitors, [105] HIV reverse transcriptase inhibitor L‐697, 661, [106] human cytomegalovirus (HCMV) inhibitors, [107] PARP inhibitors, [108] antitumor agent NSC‐693638, [109] 5‐HT3 receptor agonist [110] and ERB‐041(an estrogen receptor‐β agonist) [111] . The N ‐heterocyclic moieties are also known to be significant scaffolds in fluorescent probes [112a] .…”

Section: Synthesis Of Benzimidazole Benzoxazole and Benzothiazole Der...mentioning

confidence: 99%

Recent Advancements in Strategies for the Synthesis of Imidazoles, Thiazoles, Oxazoles, and Benzimidazoles

Kant,

Patel,

Banerjee

et al. 2023

ChemistrySelect

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Nitrogen‐containing heterocycles such as imidazoles, thiazoles, and oxazoles play a significant role in the fields of biological and pharmaceutical chemistry. These compounds were widely used for agrochemical, pesticide, medicinal, and industrial applications. Due to the wide spectrum of structural diversity as well as the biological and pharmaceutical activity of N‐heterocycles, a plethora of reports on their synthesis have appeared in the last few decades. However, developments in various bond‐forming strategies such as C−C, C−N, C−O, C−S, and N−N, as well as C−H activation, have been used as a powerful synthetic tool to derive copious N‐heterocycles. The most prominent and fascinating reports on the synthesis of imidazole, thiazole, oxazoles, and benzimidazole moieties by C−C and C−N coupling reactions, multi‐component and cycloaddition reactions, C−H activation, etc. are discussed in this study. These studies demonstrated the enormous potential of such methods for accelerating modern chemical synthesis and establishing molecular beauty through bonding. The various aspects of the methodologies, like optimized conditions, substrate scope, and mechanistic investigations, are discussed in detail.

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“…Eventually, the desired benzimidazoles were afforded by condensation of ethyl 3,4-diaminobenzoate with various sodium hydroxy(aryl)methanesulfonates (Figure 2). Utilizing the methanesulfonate compounds with different aryl substituents led to the formation of five new benzimidazoles (1)(2)(3)(4)(5). Their inhibitory effects were investigated against sirtuin enzymes (SIRT1, SIRT2, and SIRT3), and according to the results, compound 5 was found to be a pan-SIRT1-3 inhibitor.…”

Section: Inhibitors Of Histone-related Proteinsmentioning

confidence: 99%

Recent Advances in the Anticancer Applications of Benzimidazole Derivatives

Mavvaji,

Akkoc

2023

ChemistrySelect

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Cancer, one of the most deadly diseases worldwide, is still a crucial challenge to human well‐being. Hence, the design and development of modern protocols to cure diverse kinds of cancer seem highly necessary. On the other hand, benzimidazole, as an essential pharmacophore, exhibits various biological and therapeutic potency. This compound is well‐known for its pharmaceutical features, including antifungal, antiviral, antibacterial, and anticancer activities. Therefore, benzimidazole derivatives have played an essential role due to their outstanding anticancer capability, apoptotic effect, and inhibitory potential. In recent decades, numerous anticancer drug types of research have been concentrated on finding new and practical strategies for employing benzimidazole‐based compounds. This review focuses on the latest advancements and methodologies for exploiting various benzimidazole‐bearing compounds for the treatment of varied sorts of cancer, considering the mechanism of their function against cancer cell lines.

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Benzimidazole and its derivatives as cancer therapeutics: The potential role from traditional to precision medicine

Cited by 99 publications

References 187 publications

New Oxadiazole/ Benzimidazole Hybrids: Design, Synthesis, and Molecular Docking Studies.

New Oxadiazole/ Benzimidazole Hybrids: Design, Synthesis, and Molecular Docking Studies.

Recent Advancements in Strategies for the Synthesis of Imidazoles, Thiazoles, Oxazoles, and Benzimidazoles

Recent Advances in the Anticancer Applications of Benzimidazole Derivatives

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