Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors

Akhtar, Md. Jawaid; Siddiqui, Anees A.; Khan, Ahsan Ahmed; Ali, Zulphikar; Dewangan, Rikeshwer Prasad; Pasha, Santosh; Yar, Mohammad Shahar

doi:10.1016/j.ejmech.2016.12.014

Cited by 99 publications

(51 citation statements)

References 52 publications

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“…The obtained compounds were also tested for binding to EGFR and HER2 receptors. It was confirmed that their binding is analogous to the anti-cancer drug inhibiting tyrosine kinase—erlotinib [18].…”

Section: Anti-proliferative Effects Of 134-oxadiazole Derivativesmentioning

confidence: 99%

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

2018

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Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. Their anti-proliferative effects associated with various mechanisms, such as inhibition of growth factors, enzymes, kinases and others, deserve attention. The activity of these compounds was tested on cell lines of various cancers. In most publications, the most active derivatives of 1,3,4-oxadiazole exceeded the effect of reference drugs, so they may become the main new anti-cancer drugs in the future.

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Section: Anti-proliferative Effects Of 134-oxadiazole Derivativesmentioning

confidence: 99%

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

2018

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“…Staining cells with PI and Annexin V-FITC can be used as a measure of apoptotic population. Following treatment protocol as above, cells were processed for determining cellular apoptosis through flow cytometry (BD Biosciences, USA) using Annexin V-FITC Apoptosis kit (Invitrogen) as described in [ 43 ]. This assay was done following instructions protocol of the kit manufacturer.…”

Section: Methodsmentioning

confidence: 99%

9-phenyl acridine photosensitizes A375 cells to UVA radiation

Hansda

Ghosh

2020

Heliyon

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Acridines are an important class of bioactive molecules having varied uses. Its derivative, 9-phenylacridine (ACPH) had been found to exhibit antitumor activity both in cell lines and in vivo model. Its DNA binding ability and absorbance in the ultraviolet range encouraged us to investigate its role as a photosensitizer with UVA radiation. We investigated the effects of ACPH prior to UVA exposure on in vitro DNA through photo-cleavage assay. Effect of such treatment was also studied in cultured A375 melanoma cells. Endpoints studied included morphological changes, evaluation of cellular viability, scratch assay, intracellular reactive oxygen species (ROS) production, DNA damage, lipid peroxidation, glutathione (GSH) level, autophagy, cell cycle progression, depletion of mitochondrial membrane potential (ΔΨmt), induction of apoptosis and Hoechst dye efflux assay. Our findings indicated that ACPH could sensitize damage to DNA induced by UVA both in vitro and in cells. It could also potentiate cell killing by UVA. It arrested cells in G 2 /M phase and induced apoptotic death through mitochondria mediated pathway. This sensitization was through enhancement of intracellular ROS. Our findings also indicated that the stem cells side population was reduced on such treatment. The findings are important as it indicates ACPH as a promising photosensitizer and indicates its possible role in photodynamic therapy.

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“…Receptor grid generation program was run by clicking any atom of the ligand and the default box was prepared. The ligand was docked into the grid generated from the protein using extra precision (XP) and results were evaluated by glide score (docking score) program [18].…”

Section: Molecular Dockingmentioning

confidence: 99%

Formulation and evaluation of nano lipid formulation containing CNS acting drug: molecular docking, in-vitro assessment and bioactivity detail in rats

Alam

Najmi

Ahmad

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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The study performed molecular docking, formulated, characterized thymoquinone (TQ) loaded solid lipid nano particles (TQSLN) and exhibited comparative antidepressant activity. TQ loaded nano lipid formulations were prepared by solvent injection methods and characterize for different in-vitro parameters. The optimized formulation was evaluated for depression using unpredictable chronic mild stress (UCMS) model for a period of six weeks. TQSLN was assessed in modified forced swim test (MFST), tail suspension test (TST), locomotor activity followed by biochemical parameters such as monoaminesand brain derived neurotrophic factor (BDNF). The results of molecular docking study revealed that TQ has shown greater affinity and tighter binding capacity for the active site of neurotransmitter receptors. TQSLN showed nanometric size, optimum zeta potential with high percent encapsulation and lower poly dispersity index (PDI). Transmission electron microscopy (TEM) images showed spherical shape without aggregation and agglomeration of particles. The in-vivo study result revealed that the higher amount of TQ reaches to the target region by showing higher levels of monoamines 5 hydroxytryptamine (5-HT), dopamine (DA) and norepinephrine (NE) as compared to thymoquinone suspension (TQS) in brain. In conclusion, the nano lipid formulation remarkably improved the bio-efficacy of TQ and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs.

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Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors

Cited by 99 publications

References 52 publications

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

9-phenyl acridine photosensitizes A375 cells to UVA radiation

Formulation and evaluation of nano lipid formulation containing CNS acting drug: molecular docking, in-vitro assessment and bioactivity detail in rats

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