A5048968214- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Cholinesterase and Neurodegenerative Diseases
- Click Chemistry and Applications
- Quinazolinone synthesis and applications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Enzyme function and inhibition
- Antifungal resistance and susceptibility
- Inflammatory mediators and NSAID effects
- Computational Drug Discovery Methods
- Fungal Plant Pathogen Control
- Multicomponent Synthesis of Heterocycles
- Aldose Reductase and Taurine
- Synthesis of heterocyclic compounds
- Synthesis and Catalytic Reactions
- Synthesis and Reactions of Organic Compounds
- Cancer therapeutics and mechanisms
- Peptidase Inhibition and Analysis
- Insect Pest Control Strategies
- Synthesis of Tetrazole Derivatives
- Synthesis and Reactivity of Heterocycles
- Lung Cancer Treatments and Mutations
- Metal complexes synthesis and properties
- Synthesis and Characterization of Pyrroles
Eskişehir City Hospital
2015-2024
Anadolu University
2015-2024
New hybrid thiazolyl-pyrazoline derivatives (4a-k) were obtained through a facile and versatile synthetic procedure, their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I II as well acetylcholinesterase (AChE) determined. All new thiazolyl-pyrazolines showed activity at nanomolar levels hCA I, II, AChE inhibitors, with KI values in range of 13.35-63.79, 7.01-115.80, 17.89-48.05 nM, respectively....
Abstract In an effort to identify potent aldose reductase (AR) inhibitors, 5-(arylidene)thiazolidine-2,4-diones ( 1 – 8 ), which were prepared by the solvent-free reaction of 2,4-thiazolidinedione with aromatic aldehydes in presence urea, examined for their vitro AR inhibitory activities and cytotoxicity. 5-(2-Hydroxy-3-methylbenzylidene)thiazolidine-2,4-dione 3 ) was most inhibitor this series, exerting uncompetitive inhibition a K i value 0.445 ± 0.013 µM. The IC 50 compound L929 mouse...
Indole-chalcone hybrids have burst into prominence as potent weapons in the battle against pain and inflammation due to their unique features, allowing these ligands form pivotal interactions with biological targets. In this context, base-catalyzed Claisen-Schmidt condensation of 3',4'-(methylenedioxy)acetophenone heteroaromatic aldehydes carrying an indole scaffold yielded new chalcones (
New pyrazoline derivatives were synthesized and evaluated for their cytotoxic effects on AsPC-1 human pancreatic adenocarcinoma, U87 U251 glioblastoma cell lines. 1-[((5-(4-Methylphenyl)-1,3,4-oxadiazol-2-yl)thio)acetyl]-3-(2-thienyl)-5-(4-chlorophenyl)-2-pyrazoline (11) was found to be the most effective anticancer agent against lines, with IC50 values of 16.8 µM 11.9 µM, respectively. Tumor selectivity compound 11 clearly seen between Jurkat leukemic T-cell line peripheral blood...
In an effort to develop potent antidepressant agents, new pyrazoline derivatives 2a–s were synthesized and evaluated for their antidepressant-like activity by tail suspension test (TST) modified forced swimming (MFST). The effects of the compounds on spontaneous locomotor also investigated using cage apparatus. Among these derivatives, 2b, 2d, 2f, 2o, 2r decreased both horizontal vertical number mice. On other hand, 2a, 2h, 2j, 2k, 2l, 2m, 2n, which did not induce any significant change in...
In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia line that expresses Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited Abl protein kinase with IC50 value of 7.4 µM showed selective activity against positive line. Furthermore,...
In the present study, some hydrazone derivatives were synthesized via reaction of 3-cyclohexylpropionic acid hydrazide with various benzaldehydes. The chemical structures compounds elucidated by spectroscopic techniques such as IR, 1H-NMR and FAB-MS elemental analyses. evaluated for their antiinflammatory cytotoxic activities. Anti-inflammatory activity was determined in terms inhibition NF-κB, ROS generation iNOS activity. Several inhibited NF-κB iNOS, but no effect observed on...
In an attempt to develop potent anticancer agents targeting Akt, new thiazole derivatives (1–10) were synthesized and investigated for their cytotoxic effects on A549 human lung adenocarcinoma, C6 rat glioma, NIH/3T3 (healthy) mouse embryonic fibroblast cell lines. The most compounds also apoptosis Akt pathway. promising agent was found be 2-[2-((4-(4-cyanophenoxy)phenyl)methylene)hydrazinyl]-4-(4-cyanophenyl)thiazole (6), due its selective inhibitory cells with IC50 values of 12.0 ± 1.73...
In the search for small-molecule aldose reductase (AR) inhibitors, new tetrazole-hydrazone hybrids (1-15) were designed. An efficient procedure was employed synthesis of compounds 1-15. All hydrazones subjected to an in vitro assay assess their AR inhibitory profiles. Compounds 1-15 caused inhibition with Ki values ranging between 0.177 and 6.322 µM IC50 0.210 0.676 µM. 2-[(1-(4-Hydroxyphenyl)-1H-tetrazol-5-yl)thio]-N'-(4-fluorobenzylidene)acetohydrazide (4) most potent inhibitor this...
Epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) are crucial targetable enzymes in cancer management. Therefore, herein, new 2-[(5-((1H-indol-3-yl)methyl)-1,3,4-oxadiazol-2-yl)thio]-N-(thiazol/benzothiazol-2-yl)acetamides (2a–i) were designed synthesized as EGFR COX-2 inhibitors. The cytotoxic effects of compounds 2a–i on HCT116 human colorectal carcinoma, A549 lung adenocarcinoma, A375 melanoma cell lines determined using MTT assay....