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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 Jun 30 2020
Journal Name
Medico-legal Update
Effects of caring children with leukemia on their mothers` psychosocial status
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Abstract Study aim: to assess the influence of care burden for children with leukemia on their mothers` psychosocial status. Methodology: A Descriptive study, conducted at two pediatric hospitals in Baghdad city. A purposive sample of (60) mothers was participated in the study after obtaining their consent form. The instrument of the study was used to assess mothers` psychosocial status in addition to their sociodemographic characteristics. The data was processed and statistically analysed by SPSS program version 23. Result: the result of the study showed mothers have (81%) in self esteem, (77%) in psychosocial distress, (80%) for social interaction, and (76%) for social isolation. There were association between mothers` psychosocial status

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Publication Date
Sun Apr 30 2017
Journal Name
Journal Of Engineering
Implementation of a Proposed Load-Shedding System Using Altera DE2 FPGA
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A load-shedding controller suitable for small to medium size loads is designed and implemented based on preprogrammed priorities and power consumption for individual loads. The main controller decides if a particular load can be switched ON or not according to the amount of available power generation, load consumption and loads priorities. When themaximum allowed power consumption is reached and the user want to deliver power to additional load, the controller will decide if this particular load should be denied receiving power if its priority is low. Otherwise, it can be granted to receive power if its priority is high and in this case lower priority loads are automatically switched OFF in order not to overload the power generation. The

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Publication Date
Fri Dec 29 2017
Journal Name
Al-khwarizmi Engineering Journal
A Study Of Strengthening Circular Diaphragm By Ring-Shaped Concentric Ribs
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 This paper deals with the determination of stresses and deflections of clamped circular diaphragm strengthened by one or two ring-shaped concentric ribs, under uniform static and dynamic pressures. The simulation has been achieved by using the well-known engineering software finite element package MSC/NASTRAN

 As a design study, the effect of using a clamped ring, and the effect of using a ring-shaped rib on both surfaces of diaphragm instead of one, has been discussed in this work. To show the effectiveness of this study, results of this work have been compared with  published data [1].

In  the  conclusion,  the  authors underline  the  validity of  the&n

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Publication Date
Wed Sep 21 2016
Journal Name
Applicable Analysis
Retrieving the time-dependent thermal conductivity of an orthotropic rectangular conductor
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Publication Date
Wed Dec 01 2010
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
ON SOME SPECIES OF TUBULIFEROUS THRIPS (THYSANOPTERA: PHLAEOTHRIPIDAE) FROM BAGHDAD, IRAQ
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Twelve species of Tubuliferous thrips, of the family Phlaeothripidae had been reported from Iraq. Two of these were reported previously, Haplothrips cerealis Priesner, by El-Haidari and Daoud 1971 and Haplothrips tritici kurdjumov by Al-Ali 1977 and the rest were recorded for the first time: these are Haplothrips hukkineni Priesner; Haplothrips subtilissimus (Haliday); Haplothrips reuteri Karny; Haplothrips jasonis Priesner; Haplothrips sallloumensis Priesner; Haplothrips pharao Priesner; Phlaeothrips sycomri Priesner; Karnyothrips flavipus (Jones); Karnyothrips melaleucus (Bagnall); Dolicholepta micrurus (Bagnall). Number of insec

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Publication Date
Tue Sep 01 2015
Journal Name
Journal Of Engineering
Performance Enhancement of a Piezoelectric Harvester Included into an Autonomous System
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Autonomous systems are these systems which power themselves from the available ambient energies in addition to their duties. In the next few years, autonomous systems will pervade society and they will find their ways into different applications related to health, security, comfort and entertainment. Piezoelectric harvesters are possible energy converters which can be used to convert the available ambient vibration energy into electrical energy. In this contribution, an energy harvesting cantilever array with magnetic tuning including three piezoelectric bimorphs is investigated theoretically and experimentally. Other than harvester designs proposed before, this array is easy to manufacture and insensitive to manufacturi

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Publication Date
Wed Dec 30 2009
Journal Name
Iraqi Journal Of Physics
Two-dimensional Crystallization of Silica nanospheres using Coplanar DC Electric field
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Two-dimensional crystal has been achieved and controlled
with the aid of DC electric field applied between two electrodes at 5
millimeters separating distance between them. Sol-gel method has
been used to prepared nanosilica particle which used in this work as
well as TiO2 nanopaowder. The assembly of the silica particles is
due to the interaction between the electrical force, the particles
dipole, and the interaction between the particles themselves. When a
DC voltage is applied, the particles accumulated and crystallized on
the surface between the electrodes. The Light diffraction
demonstrates that the hexagonal crystal is always oriented with one
axis along the direction of the field. The particles disass

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Publication Date
Sun Mar 03 2013
Journal Name
Baghdad Science Journal
Biotreatment of AL-KARAMA Teaching Hospital Wastewater Using Aerobic Packed Bed
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This study is aimed to use the aerobic packed bed in biotreatment of the wastewater which is discharge from AL-KARAMA teaching hospital in Baghdad. The performance of packed-bed treatment method was examined for elimination of the organic compounds from wastewater under aerobic conditions. In this research different parameters were studied. They were: inoculums concentration, circulation rate of wastewater through the bed, packing type and the temperature. Results showed that the system efficiently removed about 82% of the chemical oxygen demand (COD) and 80% of the Biological oxygen demand (BOD). Percent reduction in turbidity was about 92% and reduction in nitrate concentration was about 87%. It was found that best performance of the pack

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Publication Date
Wed Nov 04 2020
Journal Name
Advances In Mobility-as-a-service Systems
Community Participation Towards Sustainability Enhancement of Transportation Sector for Baghdad City
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Crossref (2)
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Publication Date
Tue Dec 01 2009
Journal Name
Iraqi Journal Of Physics
Two-dimensional Crystallization of Silica nanospheres using Coplanar DC Electric field
...Show More Authors

Abstract:Two-dimensional crystal has been achieved and controlled with the aid of DC electric field applied between two electrodes at 5 millimeters separating distance between them. Sol-gel method has been used to prepared nanosilica particle which used in this work as well as TiO2 nanopaowder. The assembly of the silica particles is due to the interaction between the electrical force, the particles dipole, and the interaction between the particles themselves. When a DC voltage is applied, the particles accumulated and crystallized on the surface between the electrodes. The Light diffraction demonstrates that the hexagonal crystal is always oriented with one axis along the direction of the field. The particles disassemble when the field is

... Show More
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