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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 Jun 30 2021
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of the reality of applying a number of Iraqi institutional accreditation standards/study in a number of Iraqi public and private universities
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     The study aims to find out the extent to which several Iraqi institutional accreditation standards (governance and administration, scientific research, curricula) are applied in two public universities (Baghdad and Middle Technical University) and two private universities (Uruk and Al-Mansour College) by diagnosing strengths and weaknesses and proposing a mechanism and procedures to help educational institution aims to reduce or eliminate the gap. The study stems from the extent of application of several Iraqi institutional accreditation standards represented as it was worked on through observation and field coexistence to reach scientific and practical facts. The method of case study and comparison betwe

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Development of an Eco-Friendly Method for Iron Extraction and Determination in Pharmaceuticals Using Ciprofloxacin Drug as Chelating agent
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A method is developed for the determination of iron (III) in pharmaceutical preparations by coupling cloud point extraction (CPE) and UV-Vis spectrophotometry. The method is based on the reaction of Fe(III) with excess drug ciprofloxacin (CIPRO) in dilute H2SO4, forming a hydrophobic Fe(III)- CIPRO complex which can be extracted into a non-ionic surfactant Triton X-114, and iron ions are determined spectrophotometrically at absorption maximum of 437 nm. Several variables which impact on the extraction and determination of Fe (III) are optimized in order to maximize the extraction efficiency and improve the sensitivity of the method. The interferences study is also considered to check the accuracy of the procedure. The results hav

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Publication Date
Thu Jan 30 2020
Journal Name
Al-kindy College Medical Journal
Comparison between the Patterns of Common Breast Diseases Presenting as Breast Lumps in Pregnant and Non-Pregnant Married Women
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Background: Breast lump is one of the most common prevalent complaint of patients attending breast clinics.

Objective: To determine if there is any change in the pattern of common breast, diseases presenting as breast lumps between pregnant and non-pregnant women among patients attending Al-Elwiya Breast Clinic.

Methods: This is a cross – sectional study, with convent's patient sampling setting in AL-Elwiya Breast Cancer Early Detection Clinic from 1st Feb. to 1st May 2018, we collected data from patients with breast lumps including the age groups, pregnancy status, parity status, previous breast diseases, hormonal drugs, menstrual cycle, breast fe

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Publication Date
Sun Jun 01 2025
Journal Name
Results In Materials
Adsorption, thermodynamic and corrosion study of enalapril malate pharmaceutical drug as corrosion inhibitor for carbon steel in saline solution
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Unused and expired pharmaceutical drugs are a novel type of organic corrosion inhibitor. They are less expensive, more effective, and less harmful than conventional organic corrosion inhibitors. This study investigated the effects of concentration, adsorption mechanism and thermodynamic parameters of enalapril malate (ENAP) as a corrosion inhibitor for carbon steel in a saline solution (3.5 % NaCl). The polarization method was used to determine the corrosion rate and inhibition efficiency. Field emission scanning electron microscopy (FE-SEM) and atomic force spectroscopy (AFM) were used to investigate the surface morphology and topography of carbon steel after immersion in both uninhibited and inhibited media for 24 h. Fourier transform inf

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Publication Date
Wed Jul 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Automation in architecture and its effect on the regeneration of traditional buildings: Al-Shawi House as a case study
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Abstract<p>The increased applications of technology in the field of architecture, especially digital technology and aspects of automation, have made a major impact on various aspects of local architecture, especially the traditional ones. As these technologies have succeeded in integrating many technological applications in many traditional and heritage buildings and taking them to more complex uses. And included in it characteristics that were not contained, therefore the research problem was concentrated in the absence of a holistic view of the role of the aspects of automation as a technological and design effect and its mutual effects on traditional buildings (especially the traditional Bagh</p> ... Show More
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Publication Date
Sun Sep 16 2018
Journal Name
British Journal Of Educational Technology
Group tagging: Using video tagging to facilitate reflection on small group activities
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Collaborative learning in class‐based teaching presents a challenge for a tutor to ensure every group and individual student has the best learning experience. We present Group Tagging, a web application that supports reflection on collaborative, group‐based classroom activities. Group Tagging provides students with an opportunity to record important moments within the class‐based group work and enables reflection on and promotion of professional skills such as communication, collaboration and critical thinking. After class, students use the tagged clips to create short videos showcasing their group work activities, which can later be reviewed by the teacher. We report on a deployment of Group Tagging in an undergraduate Computing Scie

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Publication Date
Thu Jan 25 2024
Journal Name
Iraqi Journal Of Agricultural Sciences
EFFECTS OF MINERAL FERTILIZATION AND SPRAYING WITH SALICYLIC ACID AND AMINO ACIDS ON THE GROWTH AND PRODUCTIVITY OF INDUSTRIAL POTATOES
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This experiment was carried out at a private field in the eastern Radwaniyah Baghdad for the fall season 2020/2021 and spring 2021 to study the effects of adding mineral fertilizers, spraying salicylic acid and amino acids on some growth traits and yield of industrial potato plants. 200 kg N h-1 , 100 kg P2O5 h-1, 100 kg K2O h-1 and F2 consist of 275 kg N h-1, 180 kg P2O5 h-1, 200 K2O h-1 and F3 consist of 350 kg N h-1, 360 kg P2O5 h-1, 300 K2O h-1 and salicylic acid in three concentrations of 0,50 and 100 mg L-1 ( S1, S2, S3) and amino acids in three concentrations of 0, 1.25 and 2.5 ml L-1 ( A1, A2 , A3) It was carried out as a factorial split plot experiment, where the fertilizer levels (F1, F2 and F3) are in the main plot and th

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Publication Date
Fri Apr 26 2024
Journal Name
Annals Of The Romanian Society For Cell Biology
The response of cauliflower growth and yield to organic and chemical fertilizers application and spraying with salicylic acid
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Publication Date
Wed Jan 01 2020
Journal Name
Communications In Computer And Information Science
Performance Evaluation for Four Supervised Classifiers in Internet Traffic Classification
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Publication Date
Sat Feb 21 2026
Journal Name
Al–bahith Al–a'alami
Evaluation in the Kurdish Media Institutions (A Descriptive Study Survey)
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The importance of evaluation depends on many institutions, whether governmental or private, including media institutions, rely on the list to evaluate the weight of things and appreciation, as well as judging things, achievements, and everything related to the institution is concerned. Because through evaluation, institutions can recognize weaknesses and strengths. It is also an effective tool for management review, through which the institution can review everything related to planning and decision-making, leadership, incentives and other administrative matters.

Therefore, this study attempts to shed light on the evaluation process, its basics and its importance in general and in the Kurdish media institutions as a model in part

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