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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
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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.

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Publication Date
Tue Dec 01 2020
Journal Name
Journal Of Engineering
Performance of 2- Link Robot by utilizing Adaptive Sliding Mode Controller
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The Sliding Mode Control (SMC) has been among powerful control techniques increasingly. Much attention is paid to both theoretical and practical aspects of disciplines due to their distinctive characteristics such as insensitivity to bounded matched uncertainties, reduction of the order of sliding equations of motion, decoupling mechanical systems design. In the current study, two-link robot performance in the Classical SMC is enhanced via Adaptive Sliding Mode Controller (ASMC) despite uncertainty, external disturbance, and coulomb friction. The key idea is abstracted as follows: switching gains are depressed to the low allowable values, resulting in decreased chattering motion and control's efforts of the two-link robo

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Publication Date
Mon Jul 01 2019
Journal Name
Journal Of Engineering
Speed Controller of Three Phase Induction Motor Using Sliding Mode Controller
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In this paper, an adaptive integral Sliding Mode Control (SMC) is employed to control the speed of Three-Phase Induction Motor. The strategy used is the field oriented control as ac drive system. The SMC is used to estimate the frequency that required to generates three phase voltage of Space Vector Pulse Width Modulation (SVPWM) invertor . When the SMC is used with current controller, the quadratic component of stator current is estimated by the controller. Instead of using current controller, this paper proposed estimating the frequency of stator voltage since that the slip speed is function of the quadratic current . The simulation results of using the SMC showed that a good dynamic response can be obtained under load

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Publication Date
Sun Jun 30 2019
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Adsorption of Chromium Ions on Activated Carbon Produced from Cow Bones
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Due to the broad range uses of chromium for industrial purposes, besides its carcinogenic effect, an efficient, cost effective removal method should be obtained. In this study, cow bones as a cheap raw material were utilized to produce active carbon (CBAC) by physiochemical activation, which was characterized using: SEM to investigate surface morphology and BET to estimate the specific surface area. The best surface area of CBAC was 595.9 m2/gm which was prepared at 600 C activation temperature and impregnation ratio of 1:1.5. CBAC was used in aqueous chromium ions adsorption. The investigated factors and their ranges are: initial concentration (10-50 mg/L), adsorption time (30-300 min), temperature (20-50

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Publication Date
Wed Jun 30 2010
Journal Name
Al-kindy College Medical Journal
A prospective study of colonoscopic examination at al-kindy teaching hospital
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Background: Fiber-optic endoscopy is an important
investigation of the large intestine, whether or not the
radiologist (barium enema) has discovered a lesion in
the bowel. Colonoscopy affords a unique opportunity
to direct visualization of entire colonic mucosa. At
the same time, the physician can obtain biopsy specimens, remove polyps, and decompress volvuli.
Most experienced endoscopists and well prepared
patients can reach the cecum in over 90% of patients.
If colonoscopy is properly performed, it has a low
risk of complications, such as perforation and bleeding.
Methods: A total of 70 consecutive patients admitted
to Endoscopy department at Al-Kindy Teaching hospital from September- 2008 to July-2009.

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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Studying the Effects of Contamination on Soil Properties Using Remote Sensing
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The problem of soil contamination is increased recently due to increasing the industrial wastes such as petroleum hydrocarbon, organic solvents, and heavy metals as well as maximizing the use of agricultural fertilizers. During this period, wide development of data collection methods, using remote sensing techniques in the field of soil and environment applications appear and state the suitable technique for remediation. This study deals with the application of remote sensing techniques in geoenvironmental engineering through a field spectral reflectance measurements at nine spots of naturally hydrocarbons contaminated soil in Al-Daura Refinery Company site which is located to the south west of Baghdad using radiometer device to get stan

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Publication Date
Thu Dec 01 2016
Journal Name
Journal Of Engineering
Evaluating the Recharge of Ground Water within Al-Wand River Basin
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The estimation of recharge to ground water is the important basics to improve the use of ground water with other available resources, and to save ground water resource from depletion, especially when using large quantity of ground water during a long time such as for agricultural purposes. Al-Wand River Basin in Iraq suffers from water shortage of its requirement of Blajo–Al-Wand Project, and to cover this shortage, the ground water plays a good role to overcome this problem. In this study, three methods were used to estimate the recharge and ground water storage for Al-Wand Basin, these methods are: Water Table Fluctuation (WTF), Water Balance of Climatic for Basin, and Water Table Balance for Basin. The results showe

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Publication Date
Mon Jun 19 2023
Journal Name
Journal Of Engineering
Improvement of Soil by Using Polymer Fiber Materials Underneath Square Footing
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The change in project cost, or cost growth, occurs from many factors, some of which are related to soil problem conditions that may occurs during construction and/or during site investigation period. This paper described a new soil improvement method with a minimum cost solution by using polymer fiber materials having a length of (3 cm) in both directions and (2.5 mm) in thickness, distributed in uniform medium dense .
sandy soil at different depths (B, 1.5B and 2B) below the footings. Three square footings has been used (5,7.5 and 10 cm) to carry the above investigation by using lever arm loading system design for such purposes.
These fibers were distributed from depth of (0.1B) below the footing base down to the investigated dep

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Publication Date
Sat Sep 30 2017
Journal Name
Al-khwarizmi Engineering Journal
Thermal Conductivity Enhancement of Iraqi Origin Paraffin Wax by Nano-Alumina
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Abstract

 

Paraffin wax is utilized for the heat storage applications taking advantage from the high stored latent heat during the phase change (from solid to fluid) period. What isn't right with this procedure is that the wax has a little heat transfer rate because of its low thermal conductivity. The thermal conductivity improvement of the paraffin wax has been examined utilizing nano-material with high thermal conductivity. In the recent study, (Al2O3) nanoparticles with weights of 1, 2, and 3% of the paraffin wax were added to the paraffin wax. The Iraqi paraffin wax accessible at the local markets was utilized as a phase change material (PCM).

Many properties of the

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Publication Date
Sat Feb 09 2019
Journal Name
Iraqi Journal Of Laser
Reconstruction of 3D Shape for an Object using Laser Scanning Triangulation
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This paper presents a method of designing and constructing a system capable of acquiring
the third dimension and reconstructs a 3D shape for an object from multi images of that object using
the principle of active optical triangulation. The system consists of an illumination source, a photo
detector, a movement mechanism and a PC, which is working as a controlling unit for the hard ware
components and as an image processing unit for the object multi view raw images which must be
processed to extract the third dimension. The result showed that the optical triangulation method
provides a rapid mean for obtaining accurate and quantitative distance measurements. The final
result's analysis refers to the necessity of usin

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Publication Date
Tue Oct 01 2024
Journal Name
Science Progress
Jaw vs abdominal Burkitt's lymphoma: An analysis of 25 Iraqi cases
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This study compared the clinicopathological, immunohistochemical characteristics and Epstein-Barr virus (EBV) detection of Burkitt's lymphoma (BL) in the abdomen and jaw of Iraqi patients. A cohort/retrospective study was carried out between August and September 2024 using 25 tissue blocks (14 gnathic and 11 abdominal BL) from the Oral and Maxillofacial Laboratory, University of Baghdad, College of Dentistry, and the National Centre for Educational Laboratories. The sections were stained with haematoxylin and eosin (H&E), while CD10, CD20, Bcl-2, BCl-6, C-Myc and Ki-67 markers were used for diagnosis. The DNA detection of the EBV was performed by polymerase chain reaction (PCR). The tumours showed 22 classical and 3 atypical histologi

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