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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
Sat Jun 06 2026
Journal Name
Al–bahith Al–a'alami
FACTORS AFFECTING WOMEN’S USE OF ELECTRONIC MARKETING ON SOCIAL MEDIA : (Field Study)
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The research aims to determine the factors affecting the woman’s use of electronic marketing in social networking sites, and to know the extent of the sample’s use of social networking sites for electronic shopping purposes. The research tool used the questionnaire form that was designed in its final form after presenting it to the arbitrators and it included a set of questions and a five-Likert scale, and used the spss statistical program to perform the statistical operations that were laid out in tables showing the frequencies, percentages and percentages Salary, mean, standard deviation, and correlation using the Spearman correlation coefficient, the Ka2 square test, the F test, the Alpha Cronbach test, and arrived at Searching to

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Publication Date
Sun Aug 01 2021
Journal Name
Journal Of Mechanical Engineering Research And Developments
Slot Design Procedure for a NACA 4412 at High Angle of Attack
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The main objective of the present work is to find a method increases the efficiency of the airfoil that is used for blade in wind turbine, wing in aircraft, propeller and helicopter (like NACA 4412). By overcoming the separation of flow at high angle of attacks, a slotted airfoil had been used and solved numerically through connecting the pressure side in the bottom surface with the suction side in the top surface of the airfoil to energize the separated flow. Slot exit, width and slope were considered as a parameters of slot configuration to determine the effective design of consideration. Reynolds number was taken as [1.6 x106 ] and the angle of attacks were ranged from (0o - 20o ). The numerical solution with Ansys Fluent commercial prog

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Publication Date
Tue Nov 07 1989
Journal Name
Proc. 5th Sci.conf./src
INACTIVATION OF B*- LACTAM ANTIBIOTICS AGAINST E. COLI BY VAMIN NUTRITIONAL SUPPLEMENTION
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ABSTRACT Possible interference of vamin nutritional solution with the activity of several B-lactam antibiotics against E.coli was evaluated in vitro.In Minimal basal salts-glucose medium rapid growth inhibition of sensitive E. coli was induced by 4 µg/ml of ampicillin / cloxaillin, 8 µg/ml of ampicillin, 6 µg/ml of carbencillin, hostacillin, and cephalotin, and by 32 µg/ml of penicillin G and cloxacillin. Significant inactivation of up to 32 µg/ml of carbencillin, cephalotin, penicillin G, and hostacillin was induced by addition of 1:20 v/v vamin. This inactivation was due to the presence of specific amino acids in the mixture. Deletions of amino acids revealed that valine, leucine, isoleucine, tyrosine, tryptophan, phenylalanine, cys

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Publication Date
Wed Jan 01 2025
Journal Name
American Journal Of Biodiversity
Importance of Conventional Pap Smear Application for Iraqi women health: scientific review
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A Pap test can identify the pre-cancerous and cancerous problem in the vagina and uterine cervix. Cervical tumour is the easiest gynecologic disease to be diagnosed, treated and prevented using regular screening tests and follow-up. This review aimed to explore the opinion of specialists about cytological changes and the precancerous lesions with Pap smear test and visual inspection of the cervices, also to determine the relationship of this malignancy with demographic characteristics of patients. Results showed that few cervical cancer and pre-cancer were with women in postmenopausal period, but more were with women in the premenopausal period. Visual inspection of the cervix can show erosion lesions by gross inspection. Upon cytology exam

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Publication Date
Tue Mar 15 2016
Journal Name
Applied Research Journal
ESTIMATE THE RATIO OF TOTAL DISSOLVED SALTS FROM THE HYDROMETER TEST RESULTS
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Publication Date
Wed Dec 18 2019
Journal Name
Baghdad Science Journal
Modeling Human Capital Impact on the Development of the Iraqi Oil Industry
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Iraq has the second largest proven oil reserves in the world. According to oil experts, it is expected that the Iraq's reserves to rise to 200+ billion barrels of high-grade crude.

Oil is a strategic commodity for producing and exporting countries in general, and Iraq in particular, as demonstrated by the international experience that oil is an important means to achieve economic growth, an important tool in the overall economic, social and political development. It is also an important source of hard currency for any national economy and a means to connect the local economy and the global economy. In this paper we focus our attention on selecting the best regression model that explain the effect of human capita

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Publication Date
Thu Apr 18 2019
Journal Name
Al-kindy College Medical Journal
Congenital Club Foot Treated By Of Ponseti Method : A Short-Term Results
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Background: Congenital club foot is a complex deformity of foot .It is a collection of different abnormalities, with different etiologies. Consequently, Severity varies with   difficulties in evaluating treatment strategies with outcome results. The treatment of congenital club foot remains controversial. Usually, the orthopedist's goal is to obtain anatomically and functionally normal feet in all patients.                                Objective: To asses short term follow up result of conservatively treated club feet in relation to the age of initial casting by Ponseti technique.           Methods :A cross sectional observational study with some comparative content done in Al-kindy

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Publication Date
Sun Dec 11 2022
Journal Name
Journal Of The College Of Basic Education
Rationalization of two strength endurance tests for juniors Ages under (16) years
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Carrying strength is one of the important physical capabilities in the field of competitive sports, which affects the success of the sports training process and helps players to continue to perform skillfully, physically and tactically for as long as possible, and the capacity for endurance varies depending on the type of sports activities, it may sometimes be very short. And with a high level of intensity, such as gymnastics and wrestling movements, and it may be long, and with a medium level of intensity, as in basketball, football and other games. The research community represents a sample of Baghdad players for teams (football, basketball, handball, volleyball, wrestling, weightlifting) and for the sports season (2017-2018 AD) for ages

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Block Method for SolvingState-Space Equations of Linear Continuous-Time Control Systems
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This paper presents a newly developed method with new algorithms to find the numerical solution of nth-order state-space equations (SSE) of linear continuous-time control system by using block method. The algorithms have been written in Matlab language. The state-space equation is the modern representation to the analysis of continuous-time system. It was treated numerically to the single-input-single-output (SISO) systems as well as multiple-input-multiple-output (MIMO) systems by using fourth-order-six-steps block method. We show that it is possible to find the output values of the state-space method using block method. Comparison between the numerical and exact results has been given for some numerical examples for solving different type

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Publication Date
Wed Oct 09 2019
Journal Name
Engineering, Technology & Applied Science Research
Serviceability of Reinforced Concrete Gable Roof Beams with Openings under Static Loads
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This paper presents an analytical study on the serviceability of reinforced concrete gable roof beams with openings of different sizes, based on an experimental study which includes 13 concrete gable roof beams with openings under static loading. For deflection and crack widths under static loading at service stage, a developed unified calculation procedure has been submitted, which includes prismatic beams with one opening subjected to flexure concentrated force. The deflection has been calculated with two methods: the first method calculated deflections via relevant equations and the second was Direct Stiffness Method in which the beam is treated as a structural member with several segments constituting the portions with solid sec

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