Category: CBL Articles
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Anti-prostate cancer and anti-EGFR activities of new Nilutamide-isoxazole hybrids
Anti-prostate cancer and anti-EGFR activities of new Nilutamide-isoxazole hybrids Herein, synthesis of new Nilutamide-isoxazoles (5a-5n) via Cu(I)-promoted one-pot reaction between 1-(but-3-yn-1-yl)-5,5-dimethyl-3-(4-nitro-3-(trifluoromethyl)phenyl)imidazolidine-2,4-dione (3) and several aldehydes (4a-4n) in benign aq. tbutanol as key approach has been reported. The in vitro growth inhibition activity of all these compounds revealed that the majority of compounds were more active…
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Novel fluorinated piperazine based-amino acid derivatives as antiplasmodial agents: Synthesis, bioactivity and computational studies
Novel fluorinated piperazine based-amino acid derivatives as antiplasmodial agents: Synthesis, bioactivity and computational studies A library of twenty novel analogues of fluorinated, N-(3-hydroxy-1-phenyl-4-(4-phenylpiperazin-1-yl)alkyl)amides containing different amino acids were synthesized and tested for the activity against Plasmodium falciparum (Pf3D7) culture. All the tested compounds showed TC50 values >100 µM on HepG2 cells. Hit analogues 12c and…
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Dietary Polyphenolics: Mechanistic role in control management of Diabetes and Metabolic Syndrome
Dietary Polyphenolics: Mechanistic role in control management of Diabetes and Metabolic Syndrome The search for an antidiabetic drug is going on three fronts: technological (for instance, development of an artificial pancreas), biological (such as pancreas and islet cell transplants), and pharmacological. Our review focusses on the role of polyphenolics in pharmacological research for T2DM. Being…
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Role of Acetylcholinesterase (AChE) reactivators in the treatment of Organophosphorus poisoning: in vivo, in vitro, and in silico studies
Role of Acetylcholinesterase (AChE) reactivators in the treatment of Organophosphorus poisoning: in vivo, in vitro, and in silico studies Chemical warfare agents, especially organophosphorus (OP) compounds, are known for their extreme toxicity causing inhibition of acetylcholinesterase (AChE) enzyme activity due to covalent phosphorylation. This leads to functional impairment of muscarinic nicotinic acetylcholine receptors, resulting in…
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In-vitro evaluation of synergism in antioxidant efficiency of Quercetin and Resveratrol
In-vitro evaluation of synergism in antioxidant efficiency of Quercetin and Resveratrol Plants serve as an excellent source of therapeutic molecules that help in medicinal treatments. The production of large amounts of pure phytocompounds from plant sources for human consumption and the nature of phytocompounds exhibiting toxicity issues at higher dosages lead to the challenge of…
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Deciphering the role of c-MET in Metabolic reprogramming of Head and Neck squamous cell Carcinoma via In Silico analysis
Deciphering the role of c-MET in Metabolic reprogramming of Head and Neck squamous cell Carcinoma via In Silico analysis Targeting of epidermal growth factor receptors (EGFRs) and vascular endothelial growth factor receptors (VEGFRs) has become a major strategy for the control of head and neck cancer. c-MET, a receptor tyrosine kinase is known to be…
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Regioselective synthesis of indole-thiazolidine-2,4-dione coupled isoxazoles as in vitro tubulin polymerization inhibitors
Regioselective synthesis of indole-thiazolidine-2,4-dione coupled isoxazoles as in vitro tubulin polymerization inhibitors Herein we synthesized new indole-thiazolidine-2,4-dione coupled isoxazoles (7a-n) via simple reactions like N-propargylation, Knoevenagel condensation and copper (I) catalysed one pot regioselective reactions. All the newly synthesized compounds were characterized by 1H-NMR, 13C-NMR and Mass spectra and they were screened for in vitro…
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In Silico Docking Studies of Yucca gloriosa L. Phytoconstituents with TNF-α, IL-6 and IL-13 Receptor Against Asthma
In Silico Docking Studies of Yucca gloriosa L. Phytoconstituents with TNF-α, IL-6 and IL-13 Receptor Against Asthma Yucca gloriosa L. has been comprehensively assessed in vitro and in vivo for its action against asthma. Y. gloriosa L. is a rich source of phenolic compounds such as gloriosaols A-E and yuccaols A-E, which exhibit potent antioxidant…
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Nanoemulsion of Mentha piperita essential oil active against Mycobacterium strains
Nanoemulsion of Mentha piperita essential oil active against Mycobacterium strains Present investigation aimed to study the antimycobacterial potential of Mentha piperita essential oil fractions, identify its active constituents by GC-MS and preparation of nanoemulsion from biologically active fraction. Four oil fractions (R1, R2, R3, R4) were collected during hydrodistillation of Mentha piperiata leaves and tested…
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Development and validation of Hand-held device for the rapid detection of Metformin in biological samples: A forensic application
Development and validation of Hand-held device for the rapid detection of Metformin in biological samples: A forensic application Metformin is a widely used anti-diabetic drug that enhances glycaemic control by advancing the insulin sensitivity abatement of intestinal glucose absorption. Due to its versatility, it is also emerging as an abused drug leading to toxicity and…