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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
Fri Jun 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the effect of local exogenous application of osteopontin on wound healing in rats
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Background: Wound healing is a complex dynamical interaction between various cell types, the extracellular matrix, cytokines, and growth factors. osteoponetin is a substance that acts as an anti-inflammatory. Aims of study: The study was designed to identify the role of local exogenous applications of osteopontin on wound healing (in cheek skin). Materials and methods: Thirty adult male albino rats weighting an average of (250-300gm) used in this study, incisional wounds were made in the skin of the cheek of rat and they were divided into the following groups: A-Control group: 15 rats treated with 1µ l of normal saline B-Experimental groups: 15 rats treated with topical application of 1µl osteopontin. The scarification of animals we

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Publication Date
Wed Aug 31 2022
Journal Name
Sciencerise: Pharmaceutical Science
The morphological analysis of crystalline methadone: a novel combination of microscopy techniques
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The aim: to evaluate combined microscopy techniques for determining the morphological and optical properties of methadone hydrochloride (MDN) crystals. Materials and methods: MDN crystal formation was optimized using a closed container method and crystals were characterized using polarized light microscope (PLM), scanning electron microscopy (SEM) and confocal microscopy (CM). SEM and CM were used to determine MDN crystal thickness and study its relationship with crystal retardation colours using the Michel-Levy Birefringence approach. Results: Dimensions (mean±SD) of diamond shaped MDN crystals were confirmed using SEM and CM. Crystals were 46.4±15.2 Vs 32.0±8.3 µm long, 28.03±8.2 Vs 20.85±5.5 µm wide, and 6.62±

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Publication Date
Thu Feb 19 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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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
Mon Jan 01 2024
Journal Name
Heliyon
Synthesis and Characterization of Some Metal Ions Complexes with Mixed Ligand of Azo Dye and Metformin and Evaluation of its Effectiveness on the Growth of Some Pathogenic Bacteria Clinically Isolated and Study of its Toxicity on Normal and Cancerous Hepatocytes
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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Publication Date
Sun Sep 01 2024
Journal Name
Heliyon
Synthesis and characterization of some Metal ions complexes with mixed ligand of azo dye and Metformin and evaluation of its effectiveness on the growth of some pathogenic bacteria clinically isolated and study of its Toxicity on normal and cancerous Hepatocytes
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Four metal compounds mixed ligand of azo dye ligand (L) and metformin.(Met) were produced at aquatic ethanol for (1:1:1) (M:L:Met). The prepared compounds were identified by utilizing atomic absorption flame, FT.IR and UV–Vis spectrum manners as well as conductivity mensuration. These compounds was assayed of the gained datum the octahedral geometry was proposed into whole prepared complexes.Also in this research was studied represented examining the antibacterial and antifungal impact of the azo dye ligand (L), metformin.(Met) and (Co,Ni, Cu and Cd complexes) on four types of pathogenic, clinically isolated bacteria that are resistant to antibiotic, like Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneu

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Publication Date
Sun Oct 29 2023
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Nurses' Practices in Intensive Care Units Following Coronary Artery Bypass Grafting Patients in Baghdad City
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Objective: To evaluate nurses' practices toward coronary artery bypass grafting (CABG) patients in the
intensive care units (ICU) and to find out the relationship with some vanables.
Methodology: A purposive sample of (50) staff nurses was selected out of three hospitals for cardiac surgery.
The study instmment consisted of two major sections was constructed. It is based on the review of literature.
First it is concerned with demographic data for nurses; and the second section is observationaL tool (checklist) is
composed of six parts in which there mere (78) items. Reliability and validity of the observational checklist were
determined through the analysis of a pilot study.
Data were collected through the use of the

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