Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents

Wang, Zhe; Deng, Xin; Xiong, Runde; Xiong, Shujuan; Liu, Juan; Cao, Xuan; Lei, Xiaoyong; Chen, Yanming; Zheng, Xiaohui; Tang, Guotao

doi:10.1039/c7md00578d

Cited by 16 publications

(9 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It is reported that G1 period and S period are preparing for the presynthesis of RNA and synthesis of DNA, respectively (31). The regulation of the cell cycle is necessary to cell proliferation (33). It was found that APS exhibited an anti-proliferative effect on cancer and displayed differentiation induction on erythroid (34).…”

Section: Discussionmentioning

confidence: 99%

Astragalus polysaccharide enhances the immune function of RAW264.7 macrophages via the NF‑κB p65/MAPK signaling pathway

et al. 2020

View full text Add to dashboard Cite

The aim of the present study was to investigate the immunoregulatory effects of Astragalus polysaccharide (APS) on RAW264.7 cells. The production of cytokines by RAW264.7 cells was analyzed using ELISA, while cell viability and optimal concentration of APS were assessed using the Cell Counting Kit-8 assay. In addition, the mRNA levels of IL-6, inducible nitric oxide synthase (iNOS) and TNF-α were determined by reverse transcription-quantitative PCR analysis. The levels of co-stimulatory molecules and cell cycle distribution were assessed by flow cytometry. Electrophoretic mobility shift assay was used to determine the effects of APS on p65 expression. Compared with controls, APS enhanced the production of NO, the gene expression of TNF-α, IL-6 and iNOS and the protein levels of phosphorylated p65, p38, Jun N-terminal kinase and extracellular signal regulated kinase in RAW264.7 cells, whereas these effects of APS were alleviated by pyrrolidine dithiocarbamate. The results of the present study indicated that the immunoregulatory effects of APS are mediated, at least in part, via the activation of the NF-κB p65/MAPK signaling pathway.

show abstract

Section: Discussionmentioning

confidence: 99%

Astragalus polysaccharide enhances the immune function of RAW264.7 macrophages via the NF‑κB p65/MAPK signaling pathway

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Further, the presence of an electron-withdrawing chlorine group in the imidazole ring of benzimidazole (the R 1 position) improved antiproliferative activity compared to the positioning of an electron-donating methyl group at the same place. 72…”

Section: Anticancer Potencymentioning

confidence: 99%

“…According to SAR results, chlorine (Cl) substitution at the R 1 position, rather than the R 2 and R 3 positions, of benzimidazole improved antiproliferative activity against all the cell lines tested. Further, the presence of an electron‐withdrawing chlorine group in the imidazole ring of benzimidazole (the R 1 position) improved antiproliferative activity compared to the positioning of an electron‐donating methyl group at the same place 72 …”

Section: Anticancer Potencymentioning

confidence: 99%

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

Rostami

Haddadi

2022

Fundamemntal Clinical Pharma

View full text Add to dashboard Cite

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.

show abstract

“…The core structure of benzimidazole is a vital pharmacophore at present. It has been used as a preferred scaffold for synthesizing selected drugs of interest in medicinal chemistry, including antimicrobial [ 39 , 40 ], analgesic [ 41 ], antihelmintic [ 42 , 43 ], antioxidant [ 44 ], antimalarial [ 45 ], antiviral [ 46 ], and anticancer [ 47 ] activity. Many benzimidazole-based derivatives are available as medicines such as bendamustine, veliparib, nocodazole, liarozole, and pracinosta.…”

Section: Benzimidazole Hybridsmentioning

confidence: 99%

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

Ebenezer

Shapi

Tuszyński

2022

IJMS

View full text Add to dashboard Cite

Microtubules are cylindrical protein polymers formed from αβ-tubulin heterodimers in the cytoplasm of eukaryotic cells. Microtubule disturbance may cause cell cycle arrest in the G2/M phase, and anomalous mitotic spindles will form. Microtubules are an important target for cancer drug action because of their critical role in mitosis. Several microtubule-targeting agents with vast therapeutic advantages have been developed, but they often lead to multidrug resistance and adverse side effects. Thus, single-target therapy has drawbacks in the effective control of tubulin polymerization. Molecular hybridization, based on the amalgamation of two or more pharmacophores of bioactive conjugates to engender a single molecular structure with enhanced pharmacokinetics and biological activity, compared to their parent molecules, has recently become a promising approach in drug development. The practical application of combined active scaffolds targeting tubulin polymerization inhibitors has been corroborated in the past few years. Meanwhile, different designs and syntheses of novel anti-tubulin hybrids have been broadly studied, illustrated, and detailed in the literature. This review describes various molecular hybrids with their reported structural–activity relationships (SARs) where it is possible in an effort to generate efficacious tubulin polymerization inhibitors. The aim is to create a platform on which new active scaffolds can be modeled for improved tubulin polymerization inhibitory potency and hence, the development of new therapeutic agents against cancer.

show abstract

Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents

Cited by 16 publications

References 29 publications

Astragalus polysaccharide enhances the immune function of RAW264.7 macrophages via the NF‑κB p65/MAPK signaling pathway

Astragalus polysaccharide enhances the immune function of RAW264.7 macrophages via the NF‑κB p65/MAPK signaling pathway

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

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

Contact Info

Product

Resources

About