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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
Wed May 29 2019
Journal Name
Iraqi Journal Of Physics
Improvement the efficiency of SnO2/n-Si detector by engraving method using a CNC machine
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Tin oxide was deposited by using vacuum thermal method on silicon wafer engraved by Computer Numerical Controlled (CNC) Machine. The inscription was engraved by diamond-made brine. Deep 0.05 mm in the form of concentric squares. Electrical results in the dark were shown high value of forward current and the high value of the detection factor from 6.42 before engraving to 10.41 after engraving. (I-V) characters in illumination with powers (50, 100, 150, 200, 250) mW/cm2 show Improved properties of the detector, Especially at power (150, 200, 250) mW/cm2. Response improved in rise time from 2.4 μs to 0.72 μs and time of inactivity improved 515.2 μs to 44.2 μs. Sensitivity angle increased at zone from 40o to 65o.

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Publication Date
Mon Jun 28 2021
Journal Name
Journal Of Engineering
Effective quality control of a municipal wastewater treatment plant using Geographic information systems: A Review
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Inefficient wastewater disposal and wastewater discharge problems in water bodies have led to increasing pollution in water bodies.  Pollutants in the river contribute to increasing the biological oxygen demand (BOD), total suspended solids (SS), total dissolved solids (TDS), chemical oxygen demand (COD), and toxic metals render this water unsuitable for consumption and even pose a significant risk to human health. Over the last few years, water conservation has been the subject of growing awareness and concern throughout the world, so this research focused on review studies of researches that studied the importance of water quality of wastewater treated disposal in water bodies and modern technology to management w

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Publication Date
Mon Jun 05 2023
Journal Name
Journal Of Engineering
Serviceability behavior of High Strength Concrete I-beams reinforced with Carbon Fiber Reinforced Polymer bars
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Fiber Reinforced Polymer (FRP) bars are anisotropic in nature and have high tensile strength in the fiber direction. The use of High-Strength Concrete (HSC) allows for better use of the high-strength properties of FRP bars. The mechanical properties of FRP bars can yield to large crack widths and deflections. As a result, the design of concrete elements reinforced with FRP materials is often governed by the Serviceability Limit States (SLS). This study investigates the short-term serviceability behavior of FRP RC I-beams. Eight RC I-beams reinforced with carbon-FRP (CFRP) and four steel RC I-beams, for comparison purposes, were tested under two-point loading.
Deformations on the concrete and crack widths and spacing are measured and

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Publication Date
Thu May 25 2017
Journal Name
Genome Announcements
Complete Genome Sequence of Lytic Bacteriophage VPUSM 8 against O1 El Tor Inaba Vibrio cholerae
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ABSTRACT<p> The complete genome sequence of bacteriophage VPUSM 8 against O1 El Tor Inaba <named-content content-type="genus-species">Vibrio cholerae</named-content> is reported here. The isolated VPUSM 8 has potential use in future phage therapy or as a biocontrol agent for the prevention and treatment of cholera. </p>
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Publication Date
Wed Jan 01 2020
Journal Name
Periodicals Of Engineering And Natural Sciences
Forecasting the exchange rate of the Iraqi dinar against the US dollar using Markov chains
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Scopus
Publication Date
Wed Apr 25 2018
Journal Name
Earthquake And Structures
Response of circular footing on dry dense sand to impact load with different embedment depths
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Scopus
Publication Date
Sat Aug 21 2021
Journal Name
Engineering, Technology &amp; Applied Science Research
The Response of a Highly Skewed Steel I-Girder Bridge with Different Cross-Frame Connections
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Braces in straight bridge systems improve the lateral-torsional buckling resistance of the girders by reducing the unbraced length, while in horizontally curved and skew bridges, the braces are primary structural elements for controlling deformations by engaging adjacent girders to act as a system to resist the potentially large forces and torques caused by the curved or skewed geometry of the bridge. The cross-frames are usually designed as torsional braces, which increase the overall strength and stiffness of the individual girders by creating a girder system that translates and rotates as a unit along the bracing lines. However, when they transmit the truck’s live load forces, they can produce fatigue cracks at their connection

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Publication Date
Tue Oct 07 2003
Journal Name
University Of Baghdad
A STUDY ON SOLVENT EXTRACTION OF HOLMIUM (III) WITH SUDAN BLACK B REAGENT (M.Sc. Thesis)
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Publication Date
Wed Sep 30 2015
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Correlation of Penetration Rate with Drilling Parameters For an Iraqi Field Using Mud Logging Data
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This paper provides an attempt for modeling rate of penetration (ROP) for an Iraqi oil field with aid of mud logging data. Data of Umm Radhuma formation was selected for this modeling. These data include weight on bit, rotary speed, flow rate and mud density. A statistical approach was applied on these data for improving rate of penetration modeling. As result, an empirical linear ROP model has been developed with good fitness when compared with actual data. Also, a nonlinear regression analysis of different forms was attempted, and the results showed that the power model has good predicting capability with respect to other forms.

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Publication Date
Tue Jun 30 2015
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Using the Artificial Gas Lift to Increase the Productivity of Noor Oil Field / Mishrif Formation
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Noor Oil Field is one of Iraqi oil fields located in Missan province / Amarah city. This field is not subjected to licensing rounds, but depends on the national effort of  Missan Oil Company. The first two wells in the field were drilled in seventies and were  not opened to production until 2009. The aim of this study is to study the possibility of using the method of gas lift to increase the productivity of this field . PROSPER software was used to design the continuous  gas lift by using maximum production rate in the design.

   The design was made after comparing  the measured pressure with the calculated pressure, this comparison  show  that the method of Beggs-Brill and Petroleum Exper

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