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
Mon Apr 19 2021
Journal Name
Bridge Maintenance, Safety, Management, Life-cycle Sustainability And Innovations
Flexure strengthening of concrete bridge girders with concavely curved soffit using near-surface-mounted CFRP bars
...Show More Authors

View Publication Preview PDF
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Mon Jan 01 2018
Journal Name
Al–bahith Al–a'alami
News website Analytical: study of news sites (Iraqi Media network, The Seventh Day,Huffington Post Arabic
...Show More Authors

This research focuses on the services provided by news websites (IMN, Youm7, Huffington Post Arabic) to its audience of Internet users, as well as materials posted through its pages, trying to monitor and explain them to identify their types & features, and it›s functions, whether informational or non-informational, to know the technical potential of each of the news sites, with the entry of the latest technology information. The research used the analysis method to achieve the research objectives within the period from 1/1 to 31/1/2017. The researchers used the content analysis tool as a research tool to analyze the news sites and to know the services they provide through their pages. The research was divided into three parts, the

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sat Dec 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Application of “LIML_LVR” method practically according to the general formula K-CLASS on suggestion simultaneous equation
...Show More Authors

في هذا البحث نحاول تسليط الضوء على إحدى طرائق تقدير المعلمات الهيكلية لنماذج المعادلات الآنية الخطية والتي تزودنا بتقديرات متسقة تختلف أحيانا عن تلك التي نحصل عليها من أساليب الطرائق التقليدية الأخرى وفق الصيغة العامة لمقدرات K-CLASS. وهذه الطريقة تعرف بطريقة الإمكان الأعظم محدودة المعلومات "LIML" أو طريقة نسبة التباين الصغرى"LVR

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Nov 01 2022
Journal Name
Isa Transactions
Robust adaptive active disturbance rejection control of an electric furnace using additional continuous sliding mode component
...Show More Authors

The temperature control process of electric heating furnace (EHF) systems is a quite difficult and changeable task owing to non-linearity, time delay, time-varying parameters, and the harsh environment of the furnace. In this paper, a robust temperature control scheme for an EHF system is developed using an adaptive active disturbance rejection control (AADRC) technique with a continuous sliding-mode based component. First, a comprehensive dynamic model is established by using convection laws, in which the EHF systems can be characterized as an uncertain second order system. Second, an adaptive extended state observer (AESO) is utilized to estimate the states of the EHF system and total disturbances, in which the observer gains are updated

... Show More
View Publication
Scopus (17)
Crossref (19)
Scopus Clarivate Crossref
Publication Date
Sat Aug 01 2015
Journal Name
Journal Of Bridge Engineering
Torsional Analysis of Multicell Concrete Box Girders Strengthened with CFRP Using a Modified Softened Truss Model
...Show More Authors

Scopus (34)
Crossref (26)
Scopus Clarivate Crossref
Publication Date
Fri Sep 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
The influence of lemongrass essential oil addition into heat cured acrylic resin against Candida albicans adhesion
...Show More Authors

Background: For decades, the use of naturally accessible materials in treating human disease has been widespread. The goal of this study was to determine the anti-fungal effectiveness /of the lemongrass essential oil (LGEO) versus Candida albicans (C. albicans) adhesion to polymethylmethacrylate (PMMA) materials. Material and methods: LGEO's anti-fungal activity was tested against C. albicans adhesion using the following concentration of LGEO in PMMA monomer (2.5 vol. %, 5 vol. % LGEO) selected from the pilot study as the best two effective concentrations. A total of 40 specimens were fabricated for the candida adherence test and were subdivided into four equal groups: negative control 0 vol. % addition, experimental with 2.5 vol. % and

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (1)
Scopus Crossref
Publication Date
Thu Aug 01 2024
Journal Name
Advances In Science And Technology Research Journal
Power Predicting for Power Take-Off Shaft of a Disc Maize Silage Harvester Using Machine Learning
...Show More Authors

View Publication
Scopus (3)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Wed Jun 29 2022
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Constructed Wetland Units Filled with Waterworks Sludge for Remediating of Wastewater Contaminated with Congo Red Dye
...Show More Authors

The disposal of textile effluents to the surface water bodies represents the critical issue especially these effluents can have negative impacts on such bodies due to the presence of dyes in their composition. Biological remediation methods like constructed wetlands are more cost-effective and environmental friendly technique in comparison with traditional methods. The ability of vertical subsurface flow constructed wetlands units for treating of simulated wastewater polluted with Congo red dye has been studied in this work. The units were packed with waterworks sludge bed that either be unplanted or planted with Phragmites australis and Typha domingensis. The efficacy of present units was evaluated by monitoring of DO, Temperature, COD

... Show More
View Publication Preview PDF
Crossref (6)
Crossref
Publication Date
Sun Jan 01 2023
Journal Name
Plasma Medicine
Thermal Effect of Laser on Silver Nanoparticles Synthesized by the Cold Plasma Method on Cancer Cells
...Show More Authors

In this study, silver nanoparticles (AgNPs) were synthesized using a cold plasma technique and a plasma jet. They were then used to explore how photothermal treatment may be used to treat lung cancer (A549) and normal cells (REF) <i>in vitro</i>. The anti-proliferative activity of these nanoparticles was studied after A549 cells were treated with (AgNPs) at various concentrations (100&#37;, 50&#37;, or 25&#37;) and exposure times (6 or 8 min) of laser after 1 h or 24 h from exposed AgNPs. The highest growth inhibition for cancer cells is (75&#37;) at (AgNPs) concentration (100&#37;) and the period of exposure to the laser is (8 min). Particle size for the prepared samples varied according to the diameter o

... Show More
View Publication
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Sat Feb 01 2020
Journal Name
Journal Of Water Process Engineering
Waterworks sludge-filter sand permeable reactive barrier for removal of toxic lead ions from contaminated groundwater
...Show More Authors

Scopus (212)
Crossref (193)
Scopus Clarivate Crossref