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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 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
Sat Jan 01 2022
Journal Name
Journal Of Ecological Engineering
Biosynthetic of Titanium Dioxide Nanoparticles Using Zizyphus Spina-Christi Leaves Extract
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Crossref (12)
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Publication Date
Fri Nov 25 2022
Journal Name
Tem Journal
Preparing of ECG Dataset for Biometric ID Identification with Creative Techniques
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The Electrocardiogram records the heart's electrical signals. It is a practice; a painless diagnostic procedure used to rapidly diagnose and monitor heart problems. The ECG is an easy, noninvasive method for diagnosing various common heart conditions. Due to its unique advantages that other humans do not share, in addition to the fact that the heart's electrical activity may be easily detected from the body's surface, security is another area of concern. On this basis, it has become apparent that there are essential steps of pre-processing to deal with data of an electrical nature, signals, and prepare them for use in Biometric systems. Since it depends on the structure and function of the heart, it can be utilized as a biometric attribute

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Publication Date
Fri Oct 01 2010
Journal Name
J Saudi Soc Dermatol Dermatol Surg
Outbreak of Thallium poisoning among Iraqi Patients: A case descriptive study
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KE Sharquie, GA Ibrahim, AA Noaimi, HK Hamudy, J Saudi Soc Dermatol Dermatol Surg, 2010 - Cited by 2

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Publication Date
Sun Jun 01 2014
Journal Name
Journal Of Water Resource And Hydraulic Engineering (jwrhe)
Large Scale Field Physical Model Simulation of Roseires Dam-Break, Sudan
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Physically based modeling approach has been widely developed in recent years for the simulation of dam failure process due to the lack of field data. This paper provides and describes a physically-based model depending on dimensional analysis and hydraulic simulation methods for estimating the maximum water level and the wave propagation time from breaching of field test dams. The field physical model has been constructed in Dabbah city to represent the collapse of the Roseires dam in Sudan. Five cases of a dam failure were studied to simulate water flood conditions by changing initial water height in the reservoir (0.8, 1.0, 1.2, 1.4 and 1.5 m respectively).The physical model working under five cases, case 5 had the greatest influence of t

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Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
Job Satisfaction for Educational Counselors: General Directorate of Education Rusafa II
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The current research aims to measure the job satisfaction of educational counselors in the general directorate of education of the second Rusafa in the ministry of education of Iraq. Moreover, it aims to identify the significant differences in job satisfaction according to the gender (Male-Female), the length of service (less than 15 years more than 15 years), and the relationship between these two variables. To achieve the objectives of the research, the researcher developed a scale to measure job satisfaction. This tool was applied to sample of (100) educational counselors selected randomly. The results showed that educational counselors have job satisfaction, in which males are more satisfied in their job than females. The results als

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Publication Date
Sat Jun 01 2024
Journal Name
Baghdad Science Journal
Extraction of Caffeine from Spent Coffee Ground by Solid-liquid Extraction
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يهدف البحث الحالي إلى الاستفادة من القهوة المستهلكة , كمادة وسيطة حيث تعد القهوة المستهلكة من المخلفات المضرة للبيئة الاستخراج الكافيين الطبيعي والذي يعد مادة ذات نشاط حيوي واهمية, وتحديد العوامل الفعالة في كفاءة عملية الاستخلاص من حيث تركيز الكافيين. تضمنت المتغيرات الرئيسية المدروسة وقت الاستخلاص  0-150 دقيقة  ، ودرجة الحرارة  25-55 درجة مئوية  ، وسرعة الخلط  180-450 دورة في الدقيقة  ،   ودرجة الحموضة العالق

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Scopus (7)
Crossref (2)
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Publication Date
Sun Dec 07 2014
Journal Name
Baghdad Science Journal
Seroepidemiological Study of Measles Virus among Young Adults: Response to Revaccination
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The 2011 Iraqi Measles Control Campaign had as its aim to improve immunization coverage among young adults' 17-24years and, in the longer term, prevention of measles epidemics. The aim of the study is estimation measles vaccination and revaccination efficacy by evaluate the seroprevalence of antibody and response to reimmunization in young adults. A previously vaccinated 189 young adult medical students were tested for measles specific IgG &IgM pre and post catch-up revaccination by using commercially available ELISA. To assess the seroprevalence of antibody response pre measles reimmunization in previously vaccinated young adults; 45 were found to be seronegative. To differentiate between primary and secondary vaccine failure, anti- mea

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Crossref
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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