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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
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Women's Knowledge about Risk Factors and Early Detection of Breast Cancer at Ibn Rushd College of Education in Baghdad University
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Objective: Evaluation of women's knowledge about risk factors and early detection of breast cancer at
Ibn Rushd college of education in Baghdad University.
Methodology: The study sample included (184) women in the Ibn Rushd College / University of
Baghdad, whose age ranged between (17-58) years. Data were collected through a structured
questionnaire prepared by the National Cancer Research Center which were answered during a scientific
symposium about breast cancer. The score was calculated by correcting the results of the answer, giving
one score for each correct answer and then estimating the level of knowledge and inputting all data in a
statistical program.
Results: The results showed limited level of women's

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Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Estimation of parameters of two-dimensional sinusoidal signal model by employing Deferential Evaluation algorithm and the use of Sequential approach in estimation
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Estimation the unknown parameters of a two-dimensional sinusoidal signal model is an important and a difficult problem , The importance of this model  in modeling Symmetric gray- scale texture image . In this paper, we propose employment Deferential Evaluation algorithm and the use of Sequential approach to estimate the unknown frequencies and amplitudes of the 2-D sinusoidal components when the signal is affected by noise. Numerical simulation are performed for different sample size, and various level of standard deviation to observe the performance of this method in estimate the parameters of 2-D sinusoidal signal model , This model was used for modeling  the Symmetric gray scale texture image and estimating by using

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Publication Date
Sun Feb 28 2021
Journal Name
Journal Of Economics And Administrative Sciences
The effect of innovation and modernization as an approach to strategic change in the efficiency of organizational performance Field research in the Oil Projects Company (SCOP(
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The purpose of this research is to improve the organizational performance of the Oil Projects Company by adopting an approach to strategic change، and finding appropriate solutions to the problems facing the company. The researcher adopted in designing his research by conducting a survey of previous literature that dealt with approaches to strategic change، as the results of the survey showed that most researchers agree on the approach of renewal and modernization، Which formed a starting point for the researcher to identify the extent of the company's management interest in renewal and modernization to improve its level of performance، and the quality of the procedures followed on the ground that is related to

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Publication Date
Sun Sep 01 2019
Journal Name
Civil Engineering Journal
Effect of PolyPhosphoric Acid on Rutting Resistance of Asphalt Concrete Mixture
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The action of high repeated trucks load associated with dramatically elevated ambient temperatures leads to the most harmful distress in asphalt pavements occurred in Iraq known as rutting. Essentially, it is produced from the accumulation of irrecoverable strains, which mainly occurred in the asphalt layers. That visually demonstrated as a longitudinal depression in the wheel paths as well as small upheavals to the sides. Poly Phosphoric Acid (PPA) has been used as a means of producing modified asphalt binders and the interest to use it has increased in recent years. The PPA provides modified asphalt binder, which is relatively cheaply produced compared to polymer-modified asphalt. In this paper, PPA was used by three-percentages 1

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Comparative Study of The Amount of Apically Extrusion Of Debris During Root Canal Preparation Using Wave Oneâ„¢, Trushape 3Dâ„¢, Hyflexâ„¢ CM and One Shapeâ„¢ Instrumentation Systems (An In Vitro Study)
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Background: Many types of instruments and techniques are used in the instrumentation of the root canal system. These instruments and techniques may extrude debris beyond the apical foramen and may cause post-instrumentation complications. The aim of this study was to evaluate the amount of apically extruded debris resulted by using 4 types of nickel-titanium instruments (WaveOne, TRUShape 3D conforming files, Hyflex CM, and One Shape files) during endodontic instrumentation. Materials and methods: Forty freshly extracted human mandibular second premolar with straight canals and a single apex were collected for this study. All teeth were cut to similar lengths. Pre-weighted glass vials were used as collecting containers. Samples were randoml

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Publication Date
Tue Mar 10 2026
Journal Name
Journal Mustansiriyah Of Sports Science
The influence of excellent offensive basketball skill-learning activities based on sensory perceptions for female pupils.
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The aim of this research is to develop qualitative workouts based on certain sensory perceptions for the development of offensive basketball abilities and to determine their impact on female pupils. Several findings, based on the au-thor's extensive expertise instructing basketball materials and our closeness to the sample, revealed deficits in some sensory perceptions “in the game of basketball”, which impair the accuracy of passing the ball to the best team-mate. It also affects the pace of dribbling and the difficulty of selecting the op-timal moment and distance to fire. Therefore, the researcher designs qualita-tive activities based on many sensory experiences, including distance, speed, force, and direction shift. In addition, the

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
A study of anti fungal activity of a combination of essential oils from medical herbs against water molds
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The aim of this study is to evaluate the anti fungal activity of a combination of essential oils against water molds. HPLC analysis was done to evaluate the quantity and quality of the active compounds in this combination which extracted from three herbs( Peppermint Menthapiperita ,Thyme Thymusvulgaris, Common sage Salvia officinalis L.) and the active compounds are Camphor,Menthol,,Thujone and Thymol with different concentrations. In this study (MIC) , (MFC) were measured and (LD50) determined after 48,96 h from fingerlings treatment of common carp in aquariums .The results of (MIC) were 0.025µl/ml for Aphanomyces sp. and 0.015µl/ml for both Achlya sp. and Fusariumsolani which showed significant differences(p<0.05) from Malachite gre

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Publication Date
Tue Mar 10 2026
Journal Name
Sciences Journal Of Physical Education
Leadership patterns for university student activities managers according to the Blake and Moton model (The managerial Grid)
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The researcher is one of the workers in university sports student activities, as he noticed that there is a diversity in the use of leadership patterns among managers of student activities in Iraqi universities between one director and another, which leads to the impact of these leadership styles on performance, positive or negative, in the level of human relations and the achievement of results. The researcher adopted the descriptive method in the survey method with relational relationships. The research sample consisted of (184) sports coaches who represent (27) universities and governmental and private colleges. To achieve the research objectives, the researcher used the Statistical Package for Social Sciences (Spss). To extract.statisti

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Publication Date
Mon Mar 03 2014
Journal Name
Journal Of Baghdad College Of Dentistry
Stem Cells a Novel Approach to Periodontal Regeneration: A Review of Literature
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Publication Date
Thu Aug 03 2023
Journal Name
Cogent Arts &humanities
An Ecostylistic Analysis of Selected Extracts from Michael Punke’s Novel The Revenant
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.

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