In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents

Sathyanarayana, Reshma; Poojary, Boja; Srinivasa, Sudhanva M.; Merugumolu, Vijay Kumar; Chandrashekarappa, Revanasiddappa Bistuvalli; Rangappa, Shobith

doi:10.1007/s13738-021-02381-y

Cited by 7 publications

(6 citation statements)

References 28 publications

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“…56 Recently, Sathyanarayana et al synthesized benzimidazole derivatives containing carbon chains with variable lengths and investigated their antiinflammatory effects both in vitro and in vivo. 57 Diclofenac sodium was selected as the in vitro reference standard, and indomethacin was used as the in vivo reference drug. Among the derivatives tested, compound 21 displayed the most potent anti-inflammatory activity that was equal to that of diclofenac sodium (IC 50 = 22.54 vs. 22.72 μg/ml, respectively).…”

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

“…Based on in vitro results, six compounds were selected for in vivo examinations; all of which showed time-dependent inflammation inhibitory effects, with compound 21 being the most potent agent revealing a higher antiinflammatory activity than indomethacin within 2 h (64% vs. 53%) and 3 h (77% vs. 74%). 57 The results of SAR analysis highlighted that the anti-inflammatory activity of compound 21 would be affected by the modifications of the benzyloxy-benzylidene and alkyl moieties. The introduction of 4-Cl and 3-F on benzyloxybenzylidene enhanced anti-inflammatory activity compared with 2,4-Cl 2 (Figure 4).…”

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

“…The introduction of 4-Cl and 3-F on benzyloxybenzylidene enhanced anti-inflammatory activity compared with 2,4-Cl 2 (Figure 4). 57 Kamat et al assessed the anti-inflammatory and antibacterial activities of a number of benzimidazole tricyclic systems using bovine serum albumin degradation assay in vitro. Among the compounds screened, compound 22 (Figure 4) exhibited an inflammation inhibitory potential equal to that of the standard (IC 50 = 31.37 vs. 31.16 μg/ml, respectively).…”

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

“…Recently, Sathyanarayana et al synthesized benzimidazole derivatives containing carbon chains with variable lengths and investigated their anti‐inflammatory effects both in vitro and in vivo 57 . Diclofenac sodium was selected as the in vitro reference standard, and indomethacin was used as the in vivo reference drug.…”

Section: Anti‐inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

“…Among the derivatives tested, compound 21 displayed the most potent anti‐inflammatory activity that was equal to that of diclofenac sodium (IC 50 = 22.54 vs. 22.72 μg/ml, respectively). Based on in vitro results, six compounds were selected for in vivo examinations; all of which showed time‐dependent inflammation inhibitory effects, with compound 21 being the most potent agent revealing a higher anti‐inflammatory activity than indomethacin within 2 h (64% vs. 53%) and 3 h (77% vs. 74%) 57 . The results of SAR analysis highlighted that the anti‐inflammatory activity of compound 21 would be affected by the modifications of the benzyloxy‐benzylidene and alkyl moieties.…”

Section: Anti‐inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

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Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Rostami

Haddadi

2022

Fundamemntal Clinical Pharma

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Helicobacter pylori (H. pylori) is a microaerophilic gastric pathogen and a major contributor to chronic atrophic gastritis, peptic ulcer, and gastric malignancies. The increasing prevalence of H. pylori infection and its related diseases, such as gastric cancer (GC), motivates medicinal chemists to seek for more effective multi‐targeting drugs to prevent and treat H. pylori‐related clinical complications. Benzimidazole, a hetero‐aromatic bicyclic ring compound, has claimed a prominent role in medicinal chemistry owing to its broad range of biological activities, including antibacterial, antiviral, antidiabetic, and anticancer activities. Studies highlight the promising therapeutic potential of benzimidazole derivatives in the treatment of H. pylori‐related clinical complications such as gastric infection, gastritis, peptic ulcer, and GC. Accordingly, we here aimed to scrutinize the role of active molecules of benzimidazole derivatives as potential antibacterial, anti‐urease, anti‐inflammatory, anti‐ulcerative, and anticancer agents, which are expected to find their ways to the clinical setting sooner or later. Due to the role of structural moieties in determining the biological behaviors of benzimidazole derivatives, we explored the structure–activity relationship (SAR) of these compounds to further expand the scope of design of and research on new drugs against H. pylori‐related diseases.

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Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

Section: Anti‐inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

Section: Anti‐inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

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Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Rostami

Haddadi

2022

Fundamemntal Clinical Pharma

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Benzimidazole scaffold as a potent anticancer agent with different mechanisms of action (2016–2023)

Hagar,

Abbas,

Atef

et al. 2024

Mol Divers

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Benzimidazole scaffolds have potent anticancer activity due to their structure similarity to nucleoside. In addition, benzimidazoles could function as hydrogen donors or acceptors and bind to different drug targets that participate in cancer progression. The literature had many anticancer agents containing benzimidazole cores that gained much interest. Provoked by our endless interest in benzimidazoles as anticancer agents, we summarized the successful trials of the benzimidazole scaffolds in this concern. Moreover, we discuss the substantial opportunities in cancer treatment using benzimidazole-based drugs that may direct medicinal chemists for a compelling future design of more active chemotherapeutic agents with potential clinical applications. The uniqueness of this work lies in the highlighted benzimidazole scaffold hybridization with different molecules and benzimidazole-metal complexes, detailed mechanisms of action, and the IC50 of the developed compounds determined by different laboratories after 2015.

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Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation

Ali,

Hassan,

El Kerdawy

et al. 2024

European Journal of Medicinal Chemistry

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In vitro, in vivo and in silico-driven identification of novel benzimidazole derivatives as anticancer and anti-inflammatory agents

Cited by 7 publications

References 28 publications

Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Benzimidazole scaffold as a potent anticancer agent with different mechanisms of action (2016–2023)

Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation

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