Category: CBL Articles
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Combating Antimicrobial Resistance: A paradigm shift from general to precision medicine
Combating Antimicrobial Resistance: A paradigm shift from general to precision medicine Antimicrobial resistance (AMR) poses a significant threat to global health. It makes treating bacterial infections increasingly difficult. AMR arises from various mechanisms of antibiotic resistance including enzymatic inactivation, target alteration, efflux pumps, and decreased permeability. The limited and often ineffective treatments relying on antibiotics…
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Synthesis and biological evaluation of Trifluoromethoxyphenyl Indole Carboxamide analogs, ADME and toxicity prediction
Synthesis and biological evaluation of Trifluoromethoxyphenyl Indole Carboxamide analogs, ADME and toxicity prediction We report synthesis, ADME profile, and biological evaluation of new analogues as effective Anticancer Agents. Trifluoromethoxyphenyl indole-5-carboxamide analogues (4a-4m) were developed as a class of strong inhibitors of BCR-ABL1 kinase. The compounds (4c, 4e, and 4m) showed good anticancer activity in cancer…
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Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment
Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment Mitogen-activated protein kinases (MAPKs), also known as extracellular signal regulated kinases (ERKs), are found in numerous signal transduction pathways and are triggered by protein kinase cascades. This article will review the present state of MAPK pathway inhibitors, with…
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Remodeling of membrane lipid homeostasis in azole resistant isolates of Candida albicans
Remodeling of membrane lipid homeostasis in azole resistant isolates of Candida albicans Azole resistance mechanisms in Candida albicans infections majorly focus around the alteration of target enzymes, overexpression of efflux pump proteins, and changes in lipid metabolism. Our earlier lipidomic studies have linked changes in cellular lipid compositions to drug susceptibilities and phenotypic defects. This…
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Design, synthesis and biological evaluation of novel sulfamoyl benzamides as allosteric activators of human glucokinase
Design, synthesis and biological evaluation of novel sulfamoyl benzamides as allosteric activators of human glucokinase Glucokinase (GK) activators, which target the GK enzyme, are an emerging class of therapeutics with promising effects against diabetes. The objective of this work was to create a new group of sulfamoyl benzamide derivatives with the ability to activate GK…
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Molecular pathways with role to play in oral cancer: A mini-review
Molecular pathways with role to play in oral cancer: A mini-review Oral cancer is the sixth most prevalent type of cancer worldwide and third in India out of the different cancer types identified. Mouth and oral cancers collectively refer to cancers of the buccal cavity, lips, oropharynx, hypopharynx, and larynx. Genetic anomalies, the upregulation of…
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Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents
Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents The synthesis of new indole-oxadiazole coupled isoxazole hybrids (6a–o) synthesized by the Cu(I)-catalyzed reaction of in situ generated nitrile oxides with 3-(3,5-dichloro-4-methoxyphenyl)-5-(1-(prop-2-yn-1-yl)-1H-indol-3-yl)-1,2,4-oxadiazole in good yields have been reported here. The chemical structures of all newly synthesized hybrids were confirmed by 1H-NMR, 13C-NMR, and…
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Impact of resistin gene polymorphism on insulin resistance and Type 2 diabetes in Iraqi Babylon province patients
Impact of resistin gene polymorphism on insulin resistance and Type 2 diabetes in Iraqi Babylon province patients Resistin is cysteine-rich polypeptide produced by adipocytes and macrophages. This study aims to assess the role of resistin and its gene polymorphisms (rs-34861192 G>A, NG-023447 C>G) as potential link between obesity and insulin resistance in the development of…
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Synthesis of 1,4-disubstituted-1,2,3-Triazole derivatives for investigation of inhibition and molecular docking studies against Xanthine Oxidase
Synthesis of 1,4-disubstituted-1,2,3-Triazole derivatives for investigation of inhibition and molecular docking studies against Xanthine Oxidase This study evaluates the inhibition effect of new 1,4-disubstituted-1,2,3-triazoles against Xanthine Oxidase supplemented by molecular modelling. Nine compounds of 1,4-disubstituted-1,2,3-triazoles by Sharpless’s approach have been synthesized in this report. The structures of the synthesized compounds were characterized using FT-IR, 1H…
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Synthesis of novel phthalimide-based piperazine conjugated analogs as anti-malarial agents
Synthesis of novel phthalimide-based piperazine conjugated analogs as anti-malarial agents In the present report, we synthesized twelve novel phthalimide analogs and evaluated for antiplasmodial efficacy on Plasmodium falciparum culture. Two molecules exhibited significant inhibition percentages at 1 µM concentration without any apparent cytotoxicity on HepG2 cells. Inhibitory concentration (IC50) for both the hit compounds 6d…