Preferred Language
Articles
/
mRd8LZIBVTCNdQwC3KcL
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
...Show More Authors
Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

Scopus Clarivate Crossref
View Publication
Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
...Show More Authors

View Publication
Scopus (21)
Crossref (15)
Scopus Crossref
Publication Date
Mon Aug 01 2022
Journal Name
Baghdad Science Journal
Evaluation of Turkish Delight Prepared With Pigments And Essential Oils Extracted From Clementine (Citrus Clementine) Peels As Natural Antioxidants
...Show More Authors

This experiment presented essential oils by GC/MS, pigment content, and their antioxidant activities as well as sensory evaluation of delight samples. Limonene (66.88%) was the most prevalent yield. The peels of clementine had DPPH and ABT Scavenging activity. All levels of pigment extract had better scores for all sensory values and recorded acceptable scores in terms of appearance, color, aroma, and overall acceptability compared to control delight. Besides, delight samples containing 15 mg astaxanthin pigment extract showed maximum sensory scores compared to other samples and control delight. On the other hand, the product was less acceptable to the panelists compared to control in the case of the addition of 3.75 mg astaxanthin pigme

... Show More
View Publication Preview PDF
Scopus (5)
Crossref (4)
Scopus Clarivate Crossref
Publication Date
Mon May 02 2022
Journal Name
International Journal Of Research In Social Sciences & Humanities An International Open-access Peer Reviewed Referred Journal
Identity Construction and Social Structures in Sia Figiel’s Novel Where We Once Belonged
...Show More Authors

This article focuses on identity construction and social structures within the Sāmoan community as represented in Sia Figiel’s novel Where We Once Belonged. I argue that however the post/colonial Sāmoan identity is hybridized, the essence of the individual is still connected to Fa’a Sāmoa-the Sāmoan traditions and ways. However rapid are the colonial vicissitudes, the Sāmoan literature and lifestyle are developed to be a resistance platform. This resistance platform is dedicated not only to expose the colonial impact but also to assist the social and political reconstruction of post/colonial Samoa. To this end, this article studies identity construction, and the challenges that women face within Sāmoan social structures.

View Publication Preview PDF
Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
The risks of derivatives contracts and their reflections on the global financial crisis Analytical study in (Toronto – Dominion) bank
...Show More Authors

The research tacklets the role of risks arising from the excessive use of derivative contracts for trading in financial crises, including the recent global financial crisis in (2008) which is known the mortgage crisis.

   In order to prove the hypothesis of the research, the risk index of derivative contracts has been chosed as expressed in the measure of (value at risk) to be the main field for testing the hypothesis of research. The duration of the contract  has been also chased  for (15) years between the years (2001- 2015), the period preceding the global financial crisis, while the second represents the period of time that followed. The research reached a number of conclusions, bu

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Diacerein Loaded Novasome for Transdermal Delivery: Prepartion , In-Vitro Characterization and Factors Affecting Formulation
...Show More Authors

Diacerein (DCN) is a semi-synthetic anthraquinone derivative of Rhein that is indicated for the management of osteoarthritis. Diacerein exhibits poor dissolution in the GIT fluids and suffers from low bioavailability upon oral administration in addition to the laxative effect of Rhein metabolites. The aim of the present study was to develop novasomal vesicles with optimized entrapment efficiency and size to serve as a carrier for transdermal delivery of diacerein. Novasomal vesicles were prepared by thin film hydration method thin film hydration. The prepared vesicles were optimized utilizing different surfactant to cholesterol molar ration, sonication type, different sonication times and varying fatty acid level. The prepared vesicles were

... Show More
View Publication
Scopus (10)
Crossref (5)
Scopus Crossref
Publication Date
Wed Jul 01 2015
Journal Name
Magnetic Resonance Imaging
Alpha shape theory for 3D visualization and volumetric measurement of brain tumor progression using magnetic resonance images
...Show More Authors

Alpha shape theory for 3D visualization and volumetric measurement of brain tumor progression using magnetic resonance images

View Publication
Scopus (32)
Crossref (27)
Scopus Clarivate Crossref
Publication Date
Thu Feb 01 2024
Journal Name
Journal Of Engineering
Rutting Prediction of Asphalt Mixtures Containing Treated and Untreated Recycled Concrete Aggregate
...Show More Authors

Rutting is a crucial element of the mechanical performance characteristics of asphalt mixtures, which was the primary target of this study. The task involved substituting various portions of virgin coarse aggregate with recycled concrete aggregate materials that had been treated or left untreated at rates ranging from 25 to 100%, with a constant increase of 25%. The treatment process of recycled concrete aggregate involved soaking in acetic acid, followed by a mechanical process for a short time inside a Los Angeles machine without the balls. This research utilized two primary tests: the standard Marshall test to identify the optimal asphalt contents and the volumetric characteristics of asphalt mixtures. The other one w

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Wed May 17 2023
Journal Name
International Journal Of Computational Intelligence Systems
Prediction of ROP Zones Using Deep Learning Algorithms and Voting Classifier Technique
...Show More Authors
Abstract<p>Retinopathy of prematurity (ROP) can cause blindness in premature neonates. It is diagnosed when new blood vessels form abnormally in the retina. However, people at high risk of ROP might benefit significantly from early detection and treatment. Therefore, early diagnosis of ROP is vital in averting visual impairment. However, due to a lack of medical experience in detecting this condition, many people refuse treatment; this is especially troublesome given the rising cases of ROP. To deal with this problem, we trained three transfer learning models (VGG-19, ResNet-50, and EfficientNetB5) and a convolutional neural network (CNN) to identify the zones of ROP in preterm newborns. The dataset to train th</p> ... Show More
View Publication
Scopus (14)
Crossref (17)
Scopus Clarivate Crossref
Publication Date
Thu Nov 13 2014
Journal Name
The Iraqi Journal Of Agricultural Sciences
EFFECT OF SPRAYING SOME PLANT EXTRACTIONS AND ANTI-OXIDANT ON GROWTH AND YIELD OF SUNFLOWER
...Show More Authors

To investigate the effect of spraying some plant extraction and anti-oxidants on growth and yield of two cultivars of sunflower, a field experiment was conducted during fall season of 2009 and spring season of 2010 at the Experimental Farm, Department of Field Crop Science, College of Agriculture/ University of Baghdad. RCBD with three replications as factorial at two factors was used. First factor was cultivars Akmar and Shmoss, second was spraying with extraction of karkade at 25%, liquorices at 50%, vitamin C at concentration 1.5 mg.l-1 and nutrient which content 15 elements at concentration 15 % in addition to control treatment which sprayed with distilled water only. The result showed no significant differences between the two cultivar

... Show More
Preview PDF
Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Level of uric acid and its, relationship with lipid peroxidation in sera of patients with acute coronary syndrome
...Show More Authors

Unstable angina pectoris often leads to acute myocardial infarction. Since uric acid is thought to be risk factor for cardiovascular disease and considered a major antioxidant in human blood .The level of uric acid and lipid peroxidation in the sera of patients with unstable angina and myocardial infarction were measured and compared to the healthy individuals. Twenty-nine patients with unstable angina and twenty-nine patients with myocardial infarction were studied and compared to twenty-five healthy individuals. Uric acid was measured by using Human Kit. Malondialdelyde (MDA) a lipid peroxidation marker, was measured by thiobarbituric acid method .Significant elevation of uric acid and MDA were observed in the sera of pati

... Show More
View Publication Preview PDF
Crossref