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
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Guggulusome - A Novel Vesicular Carriers for Enhanced Transdermal Delivery
...Show More Authors

The present work describes guggul as a novel carrier for some anti-inflammatory drugs. Guggulusomes containing different concentration of guggul with aceclofenac were prepared by sonication method and characterized for vesicle shape, size, size-distribution, pH, viscosity, spread ability, homogeneity, and accelerated stability in-vitro drug permeation through mouse skin. The vesicles exhibited an entrapment efficiency of 93.2 ± 12%, vesicle size of 0.769 ± 3μm and a zeta potential of - 6.21mV. In vitro drug release was analyzed using Franz’s diffusion cells. The cumulative release of the guggulusomes gel (G2) was 75.8% in 18 hrs, which is greater than that all the gel formulation. The stability profile of prepare

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
A Novel Water Quality Index for Iraqi Surface Water
...Show More Authors

The study aims to build a water quality index that fits the Iraqi aquatic systems and reflects the environmental reality of Iraqi water. The developed Iraqi Water Quality Index (IQWQI) includes physical and chemical components. To build the IQWQI, Delphi method was used to communicate with local and global experts in water quality indices for their opinion regarding the best and most important parameter we can use in building the index and the established weight of each parameter. From the data obtained in this study, 70% were used for building the model and 30% for evaluating the model. Multiple scenarios were applied to the model inputs to study the effects of increasing parameters. The model was built 4 by 4 until it reached 17 parame

... Show More
View Publication Preview PDF
Scopus (11)
Crossref (2)
Scopus Crossref
Publication Date
Tue Aug 30 2022
Journal Name
Eurasian Chem. Commun.
Removal of some brilliant dyes by poly acrylic acid hydrogel beads
...Show More Authors

The current work discusses the removal of brilliant dyes. These dyes were Brilliant Cresyl Blue (BCB) and Brilliant Green (BG) by the use of poly acrylic acid hydrogel beads (PAA). We examined the adsorption isotherms and found that the factors preferring it are temperature and salt, shaking effects, wet PAA, (BCB) and (BG) follows Freundlich equation more than other equations. Based on the results, there is a positive correlation between adsorption of dyes (BCB and BG) and temperature (Endothermic process). We calculated the thermodynamic functions (ΔG, ΔS, and ΔH). The ion strength effects on the adsorptions at (20 °C) increased adsorption if the salt concentrations is high. We treated the kinetics outcomes based on Lagergren Equation

... Show More
Scopus (1)
Scopus
Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Spectrophotometric Determination of Ampicillin with Sulfanilic Acid by Oxidative Coupling Reaction
...Show More Authors

View Publication
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Sun Mar 30 2014
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Oxidation of Toluene to Benzoic Acid Catalyzed by Modified Vanadium Oxide
...Show More Authors

A variety of oxides were examined as additives to a V2O5/Al2O3 catalyst in order to enhance the catalytic performance for the vapor phase oxidation of toluene to benzoic acid. It was found that the modification with MoO3 greatly promoted the little reaction leading to improve catalyst performance in terms of toluene conversion and benzoic acid selectivity. The effect of catalyst surface area, catalyst promoters, reaction temperature, O2/toluene, steam/toluene, space velocity, and catalyst composition to catalyst performance were examined in order to increase the benzoic acid selectivity and yield.

View Publication Preview PDF
Publication Date
Thu Sep 30 2004
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
The Manufacture of Lead Acid Battery Separators using Locally Produced Polyethylene
...Show More Authors

View Publication Preview PDF
Publication Date
Sat Jun 30 2001
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Extraction of Iron from Al-Hussainyat Iron Ore using Acid Leaching
...Show More Authors

View Publication Preview PDF
Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Engineering
Improvement Marshall Properties of Hot Mix Asphalt Concrete Using Polyphosphoric Acid
...Show More Authors

Modified asphalt is considered one of the alternatives to address the problems of deficiencies in traditional asphalt concrete, as modified asphalt addresses many of the issues that appear on the pavement layers in asphalt concrete, resulting from heavy traffic and vehicles loaded with loads that exceed the design loads and the large fluctuations in the daily and seasonal temperatures of asphalt concrete. The current study examined the role of polyphosphoric acid (PPA) as a modified material for virgin asphalt when it was added in different proportions (1%, 2%, 3%, 4%) of the asphalt weight. The experimental program includes the volumetric characteristics associated with the Marshall test, the physical properties, and th

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Dec 01 2009
Journal Name
Journal Of Economics And Administrative Sciences
The global financial crisis and the role of war and its characterization as solutions "The objective roots and the legal possibility of the crisis in economic thought"
...Show More Authors

في البداية اود الاشارة الى ان فهم حقيقة الازمة هو ذو جانب فني يتعلق بالجينات الوراثية لنظام يملك في احيناته قدرة عالية على تفريخ المشتقات. هذا النظام الذي يزداد عقما وتدميرا يزداد قدرة على خلق النقود الائتمانية/المشتقات، وكلما اقتربنا اكثر من فهم هذا الجانب كلما اسقطت في ايدينا تلك التوصيفات الاكاديمية الجاهزة في نقص الرقابة والاشراف، تركيز المخاطر،....الخ التي تناولتها الكتابات الشائعة في معظم طروحات

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Jun 01 2018
Journal Name
Journal Of The College Of Languages (jcl)
L’imaginaire de l’épidémie dans La Peste d’Albert Camus et Le Choléra de Nazik al-Malaika The Imagination of Epidemic in Alber Kamo's Novel " Plague" and Nazik Al-Malaekah's poem "Cholera"
...Show More Authors

The present study deals with the story of Epidemic in two literary works issued in the same year (1947). One of them is a novel titled "Plague" written by the French writer Alber Kamo, the second is a poem of the Iraqi poetess Nazik Al-Malaekah. The research reflects a contrastive study of the war vision in the two works as both writers used science to serve literature by using Epidemic as a metaphor to refer to the dangers that the societies faced.

The problem of the present research lies in answering the question about the reason that makes the two writers use metaphor while narrating the issues of the society instead of mentioning them directly and illuminate what implications do the narrative style of Epidemic story have and

... Show More
View Publication Preview PDF