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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 Jun 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
The role of governance in the evaluation of the social performance of the economic units
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The aim of this investigation is to study and analysis the role of governance in the evaluation of the and social performance of the economic units to be addressed through the concept of corporate governance and then to the social performance and its relationship to corporate governance.

The most important obtained results from this research is that the corporate governance of extreme importance, and derive their importance from being an essential tool to contribute to the transparency and fair disclosure of the financial results of economic units in the fight against financial and administrative corruption in economic units, thus providing protection and confidence of all parties, and the evaluating soci

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Publication Date
Sat Sep 01 2018
Journal Name
Iraqi Journal Of Science
Estimate Antimicrobial activity and Anti-biofilm formation of bark Cinnamomum zeylanicum on Klebsiella pneumoniae isolated from Urinary Tract Infections
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Publication Date
Mon Jun 05 2023
Journal Name
Journal Of Engineering
Prediction of Compressive Strength of Reinforced Concrete Structural Elements by Using Combined Non-Destructive Tests
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This research is devoted to investigate relationship between both Ultrasonic Pulse Velocity and Rebound Number (Hammer Test) with cube compressive strength and also to study the effect of steel reinforcement on these relationships.
A study was carried out on 32 scale model reinforced concrete elements. Non destructive testing campaign (mainly ultrasonic and rebound hammer tests) made on the same elements. About 72 concrete cubes (15 X 15 X15) were taken from the concrete mixes to check the compressive strength.. Data analyzed.Include the possible correlations between non destructive testing (NDT) and compressive strength (DT) Statistical approach is used for this purpose. A new relationships obtained from correlations results is give

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Publication Date
Tue Jan 01 2019
Journal Name
Plant Archives
Effect of the addition of guanidinoacetic acid to the dilute tris in some of the biochemical characteristics of the semen of the rams
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The study was planned to evaluate the effect of adding Guanidinoacetic acid in some characteristics of the sperm of the rams. This study was conducted in the animal field of the Animal Production Department / Faculty of Agricultural Engineering Sciences / University of Baghdad, for the period from 5/8/2018 to 28/2/2019. In this experiment, 3 rams were used at the age of 2-2.5 years and weighed 50-54 kg. The semen was collected early in the morning and once a week and the semen was pooled to remove the individual differences. The treatments were divided: GAA-free control group, treatment T1 (0.05 mg / 100 ml GAA), T2 treatment (0.1 mg / 100 ml GAA) and T3 treatment (0.2 mg / 100 ml GAA). The results of the study showed a significant decrease

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Publication Date
Wed Jul 30 2025
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Comprehensive Molecular Profiling of the 3′UTR Region of the CEBPA Gene in Iraqi Patients with Acute Myeloid Leukemia Reveals Novel Regulatory Variants
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Background: Acute myeloid leukemia (AML) is a genetically heterogeneous leukemia characterized by abnormal myeloid blast accumulation, disrupting normal hematopoiesis and leading to rapid progression. Objective: To investigate SNPs within the 3’UTR of the CCAAT/enhancer-binding protein alpha (CEBPA) gene and its association with AML in Iraqi patients. Methods: The study was carried out on 120 AML patients classified into newly diagnosed, induction chemotherapy, and consolidation chemotherapy stages (40 each), and 40 individuals as a control group. Genomic DNA was extracted from AML patients and controls, followed by PCR amplification and Sanger sequencing of the 3’UTR region of the CEBPA gene. The AML patients were characterized

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Publication Date
Mon Jan 01 2024
Journal Name
5th International Conference On Biomedical And Health Sciences
Exploiting Vpusm 8 Lytic Phage for The Bio- Control of V. Cholerae: A Novel Approach Against Cholera in The Era of Antibiotic Resistance
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Objective: The purpose of this study was to assess the effectiveness of Vibriophage Universiti Sains Malaysia 8 (VPUSM 8), a bacteriophage that destroys bacteria, in managing the proliferation of Vibrio cholerae, specifically the El Tor serotype, as an alternate therapeutic strategy. Methods: The study entailed subjecting water samples from Kelantan, Malaysia, to reproduce the natural circumstances that promote the growth of V. cholerae. Subsequently, the samples were contaminated with the V. cholerae O1 El Tor Inaba strain and treated using VPUSM 8. The study employed a controlled experimental design, wherein the samples were divided into three groups, each experiencing different treatment methods. Quantifying the number of colony-

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Publication Date
Thu Apr 01 2021
Journal Name
Computer Methods And Programs In Biomedicine
A hybrid approach based on multiple Eigenvalues selection (MES) for the automated grading of a brain tumor using MRI
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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
Anti-Social behavior and its relationship to the need to love at Baghdad University students
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1. Anti-social behavior Baghdad University students.
2. Know the differences in anti's social behavior according to gender, specialization.
3. Know-the need for love at Bagdad University students.
4. Know the relationship between anti-social behavior and the need to love.
The research sample consisted of (100) students, the researcher numbers tools to measure anti behavior and the need to love.
The results showed that college students have an anti-social behavior is weak and they need to love and there is no correlation between them Function relationship. Researcher has shown a number of recommendations and proposals.

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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of The College Of Education For Women
Adnan Al-Sayegh's Anti-War Poetry: A Cry Against Inhumanity
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This paper aims at exploring the impact of the Iraq-Iran war in the poetry of Adnan Al-Sayegh. Al-Sayegh participation in this war makes him a first hand witness to the atrocities of the trenches and fight in the first lines. This war did not only change his life and world view for good, it changes the nature of his poetry as well. As aresult, war becomes a central issue not only in the poetry Al-Sayegh wrote in the 1980s and 1990s Iraq, but also in the exile.
Key Words: War, Al-Sayegh, Poetry.

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Publication Date
Sun Mar 08 2026
Journal Name
Journal Of Baghdad College Of Dentistry
In vivo histological evaluation of the effect of the topical application of estrogen hormone on wounds healing in ovariectomized rabbit
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Background: Wound healing, as a normal biological process in the human body, is achieved through four precisely and highly programmed phases: hemostasis, inflammation, proliferation, and remodeling. Growth factors released in the traumatized area promote cell migration into the wound area (chemotaxis), stimulate the growth of epithelial cells and fibroblasts (mitogenesis), initiate the formulation of new blood vessels (angiogenesis), and stimulate matrix formation and remodeling of the affected region. One of factors that effects on wound healing is a sex hormones and one of these hormones is an estrogen hormone. A wide range of cutaneous cell types (eg, fibroblast, endothelial, epithelial, and inflammatory) expressed estrogen receptors, in

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