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View article: Development and Biological Assessment of Thiazole-Based Pyridines for Targeted Therapy in Lung Cancer
Development and Biological Assessment of Thiazole-Based Pyridines for Targeted Therapy in Lung Cancer Open
The study aims to synthesize, characterize, and evaluate a series of novel compounds for their potential anticancer activity targeting the A549 lung cancer cell line. The hydrazonothiazole-based pyridine compounds (2a-2o) were characterize…
View article: Design, synthesis of novel thiazole‐thiomorpholine derivatives and evaluation of their anticancer activity via in vitro and in silico studies
Design, synthesis of novel thiazole‐thiomorpholine derivatives and evaluation of their anticancer activity via in vitro and in silico studies Open
Continuous efforts are carried out to find new cancer treatments. Compounds including thiazole or thiomorpholine rings showed favorable biological activities for various diseases including cancer. In this study, a new series of 4‐(4‐{[2‐(4…
View article: Comparison of apoptotic effects of lupeol on A549 and C6 cell lines
Comparison of apoptotic effects of lupeol on A549 and C6 cell lines Open
Lupeol compound is a cyclic triterpene alcohol that is widely found in plants. The compound lupeol has been reported to exhibit antitumor, anti-inflammatory, anxiolytic, neuroprotective and hepatoprotective effects. Recent research shows t…
View article: COX inhibitory profiles of a series of thiadiazole-benzothiazole hybrids
COX inhibitory profiles of a series of thiadiazole-benzothiazole hybrids Open
In an endeavour to identify small molecule COX-1 inhibitors, a colorimetric assay protocol was applied for the in vitro evaluation of COX-1 and 2 inhibitory potential of a series of thiadiazole-benzothiazole hybrids. The most potent and se…
View article: Synthesis of Some New 1,3,4-Oxadiazole Derivatives and Evaluation of Their Anticancer Activity
Synthesis of Some New 1,3,4-Oxadiazole Derivatives and Evaluation of Their Anticancer Activity Open
In this work, some new 2-[(5-((2-acetamidophenoxy)methyl)-1,3,4-oxadiazol-2-yl)thio]acetamide derivatives (4a-4l) were synthesized and studied for their anticancer activity. Twelve new compounds were tested on the A549 human lung cancer ce…
View article: Screening of new morpholine dithiocarbamate derivatives bearing benzimidazole moiety for anticholinesterase potential
Screening of new morpholine dithiocarbamate derivatives bearing benzimidazole moiety for anticholinesterase potential Open
Alzheimer’s disease (AD) is basically associated with disturbances of cholinesterase metabolism which result in acetylcholine deficiency. Target of acetylcholinesterase (AChE) inhibitors used in symptomatic therapy of disease is to increas…
View article: Discovery of Small Molecule COX-1 and Akt Inhibitors as Anti-NSCLC Agents Endowed with Anti-Inflammatory Action
Discovery of Small Molecule COX-1 and Akt Inhibitors as Anti-NSCLC Agents Endowed with Anti-Inflammatory Action Open
Targeted therapies have come into prominence in the ongoing battle against non-small cell lung cancer (NSCLC) because of the shortcomings of traditional chemotherapy. In this context, indole-based small molecules, which were synthesized ef…
View article: Origanum minutiflorum O. Schwarz et P. H. Davis essential oil: enzyme inhibitory activities and chemical composition
Origanum minutiflorum O. Schwarz et P. H. Davis essential oil: enzyme inhibitory activities and chemical composition Open
The essential oil (EO) of Origanum minutiflorum O. Schwarz et P. H. Davis was obtained by the hydrodistillation method. The analysis of the EO was conducted using Gas Chromatography (GC) and Gas Chromatography/Mass Spectrometry (GC/MS). Th…
View article: Origanum minutiflorum O. Schwarz et P. H. Davis essential oil: enzyme inhibitory activities and chemical composition.
Origanum minutiflorum O. Schwarz et P. H. Davis essential oil: enzyme inhibitory activities and chemical composition. Open
The essential oil (EO) of Origanum minutiflorum O. Schwarz et P. H. Davis was obtained by the hydrodistillation method.The analysis of the EO was conducted using Gas Chromatography (GC) and Gas Chromatography/Mass Spectrometry (GC/MS).The …
View article: Microwave-assisted synthesis of a series of 4,5-dihydro-1H-pyrazoles endowed with selective COX-1 inhibitory potency
Microwave-assisted synthesis of a series of 4,5-dihydro-1H-pyrazoles endowed with selective COX-1 inhibitory potency Open
Considerable efforts have been directed towards the discovery of selective cyclooxygenase isoxyme 1 (COX-1) inhibitors due to the recent work highlighting the involvement of COX-1 in the pathogenesis of pain, neuroinflammation, cancer and …
View article: Acetylcholinesterase Inhibitor Activity of Some 5-Nitrothiophene-Thiazole Derivatives
Acetylcholinesterase Inhibitor Activity of Some 5-Nitrothiophene-Thiazole Derivatives Open
The potential anticholinesterase characteristics of some thiazole derivatives (2a–2j), including the 5-nitrothiophene moiety, were examined in this work. 1H-NMR, 13C-NMR, and HRMS spectral data were used to determine the structure of the c…
View article: <i>In vitro</i> evaluation of 2-pyrazoline derivatives as DPP-4 inhibitors
<i>In vitro</i> evaluation of 2-pyrazoline derivatives as DPP-4 inhibitors Open
Objectives In this study, the synthesis of three pyrazoline derivatives and the evaluation of their inhibitory effects on dipeptidyl peptidase (DPP-4) were aimed. Methods Pyrazoline-based compounds (1–3) were obtained via the reaction of 1…
View article: Design, Synthesis and In vitro COX Inhibitory Profiles of A New Series of Tetrazole-based Hydrazones
Design, Synthesis and In vitro COX Inhibitory Profiles of A New Series of Tetrazole-based Hydrazones Open
Inhibition of cyclooxygenases (COXs), by selective and nonselective inhibitors, is a favorable approach for pharmacologic intervention in a variety of disorders such as cancer. For this purpose, a new class of tetrazole-hydrazone hybrids (…
View article: Synthesis of New 1,2,4-Triazole Derivatives and Investigation of Their Matrix Metalloproteinase-9 (MMP-9) Inhibition Properties
Synthesis of New 1,2,4-Triazole Derivatives and Investigation of Their Matrix Metalloproteinase-9 (MMP-9) Inhibition Properties Open
Nine new 2- [[5-((4-acetamidophenoxy)methyl)-4-phenyl-4H-1,2,4-triazol-3-yl] thio]-N-(aryl/heteroaryl)acetamide (5a-5i) derivatives were synthesized and tested for their matrix metalloproteinase-9 (MMP-9) inhibition potency which is associ…
View article: Evaluation of new sulfathiazole derivatives as antiproliferative agents
Evaluation of new sulfathiazole derivatives as antiproliferative agents Open
Objectives Sulfonamide group is an important scaffold used for generating new building blocks with diverse biological activities. Considering priority of the sulfonamide structure, seven new sulfathiazole derivatives were synthesized and e…
View article: <i>In vitro</i> and <i>in silico</i> studies on AChE inhibitory effects of a series of donepezil-like arylidene indanones
<i>In vitro</i> and <i>in silico</i> studies on AChE inhibitory effects of a series of donepezil-like arylidene indanones Open
Objective Donepezil is the most potent acetylcholinesterase (AChE) inhibitor currently available on the market for the management of Alzheimer’s disease. In this study, it was aimed to identify potent donepezil analogues. Materials and met…
View article: Synthesis and Biological Evaluation of Some New Hydrazone Derivatives Bearing Pyrimidine Ring as Analgesic and Anti-Inflammatory Agents
Synthesis and Biological Evaluation of Some New Hydrazone Derivatives Bearing Pyrimidine Ring as Analgesic and Anti-Inflammatory Agents Open
New hydrazone derivatives were synthesized from 4-chloro-2-(methylthio) pyrimidine-5-carbohydrazide. IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis characterized synthesized compounds. All compounds were investigated for an…
View article: Synthesis and evaluation of new benzoxazole derivatives as potential antiglioma agents
Synthesis and evaluation of new benzoxazole derivatives as potential antiglioma agents Open
Gliomas account for the majority of human brain tumors and the incidence of gliomas is expected to rise in upcoming years and therefore extensive efforts have been devoted to the discovery of potent antiglioma agents.Due to the importance …
View article: Synthesis and evaluation of new benzoxazole derivatives as potential antiglioma agents
Synthesis and evaluation of new benzoxazole derivatives as potential antiglioma agents Open
Gliomas account for the majority of human brain tumors and the incidence of gliomas is expected to rise in upcoming years and therefore extensive efforts have been devoted to the discovery of potent antiglioma agents. Due to the importance…
View article: Synthesis and Evaluation of A New Series of Thiazolyl-Pyrazoline Derivatives as Cholinesterase Inhibitors
Synthesis and Evaluation of A New Series of Thiazolyl-Pyrazoline Derivatives as Cholinesterase Inhibitors Open
In the view of this study, the structural modification of the identified compounds is on-going for the generation of new cholinesterase inhibitors with enhanced efficacy.
View article: New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation
New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation Open
In this study, novel N′-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3H)-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide (4a–4k) derivatives were synthesized and their anticancer potency were evaluated on human b…
View article: Synthesis and Evaluation of New Oxadiazole, Thiadiazole, and Triazole Derivatives as Potential Anticancer Agents Targeting MMP-9
Synthesis and Evaluation of New Oxadiazole, Thiadiazole, and Triazole Derivatives as Potential Anticancer Agents Targeting MMP-9 Open
Matrix metalloproteinases (MMPs) are important proteases involved in tumor progression including angiogenesis, tissue invasion, and migration. Therefore, MMPs have been reported as potential diagnostic and prognostic biomarkers in many typ…
View article: Novel benzothiazole based imidazole derivatives as new cytotoxic agents against glioma (C6) and liver (hepG2) cancer cell lines
Novel benzothiazole based imidazole derivatives as new cytotoxic agents against glioma (C6) and liver (hepG2) cancer cell lines Open
Cancer is the second leading cause of death after heart disease throughout the world.A great amount of anticancer drugs are discovered and still have been designed nowadays for cancer treatment 1 .Today, treatments involving cytotoxic drug…
View article: Synthesis and Evaluation of New Benzodioxole- Based Thiosemicarbazone Derivatives as Potential Antitumor Agents
Synthesis and Evaluation of New Benzodioxole- Based Thiosemicarbazone Derivatives as Potential Antitumor Agents Open
New benzodioxole-based thiosemicarbazone derivatives were synthesized and evaluated for their cytotoxic effects on A549 human lung adenocarcinoma, C6 rat glioma and NIH/3T3 mouse embryonic fibroblast cells. In order to examine the correlat…
View article: Novel tetrazole derivatives: synthesis, anticholinesterase activity and cytotoxicity evaluation
Novel tetrazole derivatives: synthesis, anticholinesterase activity and cytotoxicity evaluation Open
Objective(s) The synthesis of new N′ -arylidene-4-[(1-phenyl-1 H -tetrazole-5-yl)thio]butanoylhydrazide derivatives ( 1–26 ) and investigation of their potential anticholinesterase (AChE), butyrylcholinesterase (BuChE) enzyme inhibition ac…
View article: Chemical characterization and anticholinesterase effects of essential oils derived from <i>Salvia</i> species
Chemical characterization and anticholinesterase effects of essential oils derived from <i>Salvia</i> species Open
Inhibitory effect of Salvia species herbal preparations on acetylcholinesterase (AChE) and butylcholinesterase (BuChE) activitiy may contribute to regulation of cognitive performance and impaired cholinergic functions in patients with Alzh…
View article: Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents
Synthesis of novel 3, 5, 6-trisubstituted triazine derivatives and their biological activity evaluation as potential antitumor and anti-inflammatory agents Open
In this study, new 3, 5, 6-trisubstituted 1, 2, 4-triazine derivatives (1-9) were synthesized and their structures were determined by using NMR, IR and Mass spectroscopic methods.In vitro antitumor activities against MCF-7 breast adenocarc…
View article: Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives
Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives Open
Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivative…