A5059408488- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Alzheimer's disease research and treatments
- Synthesis and Characterization of Heterocyclic Compounds
- Pesticide Exposure and Toxicity
- Nicotinic Acetylcholine Receptors Study
- Biochemical Acid Research Studies
- Effects and risks of endocrine disrupting chemicals
- Medicinal Plants and Neuroprotection
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Liver physiology and pathology
- Cancer Mechanisms and Therapy
- Chemical synthesis and alkaloids
- Inflammatory mediators and NSAID effects
- Graphene and Nanomaterials Applications
- Synthesis of Tetrazole Derivatives
- Enzyme function and inhibition
- Sulfur-Based Synthesis Techniques
- Phenothiazines and Benzothiazines Synthesis and Activities
- Nanoparticle-Based Drug Delivery
- Drug-Induced Hepatotoxicity and Protection
- Drug Transport and Resistance Mechanisms
- Cancer-related Molecular Pathways
Hacettepe University
2015-2025
Adıyaman University
2014
University of Pecs
2014
University "St. Kliment Ohridski" - Bitola
2014
Bellvitge University Hospital
2014
University of Montana
2010-2011
University of California, San Diego
2011
In order to find novel cyclooxygenase (COX)‐2 inhibitors for treating inflammatory‐based diseases such as Alzheimer's disease (AD), an ethyl carboxylate side chain was added 5‐(4‐chlorophenyl)‐6‐(4‐(methylsulfonyl)phenyl)‐3‐(methylthio)‐1,2,4‐triazine (lead compound II ) maintain residual inhibition of COX‐1 through interacting with Arg120. A preliminary molecular docking study on both the COX‐1/COX‐2 active sites truly confirmed our hypothesis. Accordingly, a series...
A novel series of coumarin derivatives linked to the N-benzyl triazole group were synthesized and evaluated against 15-lipoxygenase (15-LOX), acetyl- butyrylcholinesterase (AChE BuChE) find most potent derivative Alzheimer's disease (AD). Most compounds showed weak moderate activity ChEs. Among active BuChE 15-LOX inhibitors, 8l 8n exhibited an excellent neuroprotective effect, higher than standard drug (quercetin) on PC12 cell model injured by H2O2 significantly reduced aggregation amyloid...
In this research, a series of coumarin-based scaffolds linked to pyridine derivatives via flexible aliphatic linkage were synthesized and assessed as multifunctional anti-AD agents. All the compounds showed acceptable acetylcholinesterase (AChE) inhibition activity in nanomolar range (IC50 = 2-144 nM) remarkable butyrylcholinesterase (BuChE) property 9-123 compared donepezil standard drug 14 275 nM, respectively). Compound 3f best AChE inhibitor 2 BuChE 24 nM), 100 times more active than...
Abstract Bisphenol A (BPA) is an endocrine disruptor chemical, which commonly used in everyday products. Adverse effects of its exposure are reported even at picomolar doses. Effects and nanomolar concentrations BPA on cytotoxicity, nitric oxide (NO) levels, acetylcholinesterase (AChE) gene expression activity, tumor necrosis factor‐α (TNF‐α) caspase‐8 levels were determined SH‐SY5Y cells. The current study reveals that low‐dose treatment induced NO, We also evaluated the mechanism...
Two series of novel coumarin derivatives, substituted at 3 and 7 positions with aminoalkoxy groups, are synthesized, characterized, screened. The effect amine substituents the length cross-linker investigated in acetyl- butyrylcholinesterase (AChE BuChE) inhibition. Target compounds show moderate to potent inhibitory activities against AChE BuChE. 3-(3,4-Dichlorophenyl)-7-[4-(diethylamino)butoxy]-2H-chromen-2-one (4y) is identified as most compound (IC50 =0.27 μm). Kinetic molecular modeling...
Aim: Mesenchymal-epithelial transition factor (c-Met)/HGF overactivation is involved in diverse human cancers. Materials & methods: Herein, we report the synthesis and biological evaluation of thiomethylpyridine-linked triazolotriazines as c-Met kinase inhibitors. Results: Compounds 10b 11e were more potent than crizotinib on HepG2 cells with IC50 values 0.74 0.71 μM MTT assay, respectively. Interestingly, all target compounds displayed range 3.9-11.1 nM inhibition assay which lower value...
Background: Since the binding of estradiol to its receptor promotes breast cancer cell proliferation (in ER+ tumours), many molecules targeting this protein have been synthesized counteract action. Ferrocene derivatives proved their efficiency against hormone-dependent cells (MCF-7). Objective: In study, we aimed find new ferrocene having pharmacochemistry properties as potential drugs human cells. Methods: A series 29 N-ferrocenylmethylaniline A0-A28 were synthesised, and anti-proliferative...
Abstract Hepatocellular carcinoma is the most common type of primary liver cancer. However, multidrug resistance (MDR) a major obstacle to effective chemotherapy cancer cells. This report documents rational design, synthesis, and biological evaluation novel series triazolotriazines substituted with CH 2 NH‐linked pyridine for use as dual c‐Met/MDR inhibitors. Compound 12g IC 50 3.06 μM on HepG2 cells showed more potency than crizotinib (IC = 5.15 μM) in MTT assay. In addition, inhibited...