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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
Tue Jan 03 2023
Journal Name
College Of Islamic Sciences
Narrative Structures in the Novel “Qiamat Baghdad” for the Novelist Alia Talib – Semiotic Study
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Abstract

The human mind knew the philosophy and logic in the ancient times, and the history afterwards, while the semiotics concept appeared in the modern time, and became a new knowledge field like the other knowledge fields. It deals, in its different concepts and references, with the processes that lead to and reveals the meaning through what is hidden in addition to what is disclosed. It is the result of human activity in its pragmatic and cognitive dimensions together. The semiotic token concept became a knowledge key to access all the study, research, and  investigation fields, due to its ability of description, explanation, and dismantling. The paper is divided into two sections preceded by a the

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Publication Date
Wed Mar 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of adding titanium dioxide nanoparticles on anti-microbial activity and surface detail reproduction of dental alginate
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Most dental works require a diagnostic impression; alginate is contemplated as the most popular material used for this purpose. Titanium dioxide nanoparticles show evidence of antimicrobial activity in the recent era, for this purpose, this study aimed to evaluate the effect of adding Titanium dioxide nanoparticles on antimicrobial activity and surface detail reproduction of alginate impression material. Materials and methods: Titanium dioxide nanoparticles (purity = 99%, size= 20nm) was added to alginate at three different concentrations (2%, 3% and 5%). 84 samples were prepared in total. Samples were tested for antimicrobial activity using a disc diffusion test, and surface detail reproduction was done using (ISO 21563:2021). One-way A

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Publication Date
Mon Mar 02 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The Effects of Nano-Hydroxyapatite and Casein Phosphopeptide-Amorphous Calcium Phosphate in Preventing Loss of Minerals from Teeth after Exposure to an Acidic Beverage (An In vitro Study)
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Background: To evaluate the effect of antierosive agents (10% Nano-Hydroxyapatite (NHA), 10% Casein Phophopeptide-Amorphous Calcium Phosphate (CPP-ACP), and combination of 10% NHA and 10% CPP-ACP) on loss of minerals from enamel surface of permanent teeth treated with antierosive agents when exposed to an acidic beverage and investigate the morphological changes of treated enamel surface after demineralization with cola based beverage under Scanning Electron Microscope (SEM). Materials and Methods: Sixty maxillary first premolars were randomly divided into four groups, 15 teeth for each group. Group I treated with 10% NHA, Group II treated with 10% CPP-ACP, Group III treated with 10% NHA and 10% CPP-ACP, and Group IV did not treat with any

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Publication Date
Mon Apr 04 2022
Journal Name
Journal Of Research In Medical And Dental Science
Efficacy of Varnishes with: Bioactive Glass, Recaldent Technology and Silver Diamine Fluoride in Comparison with Sodium Fluoride on Tooth Surface Micro-hardness (an In Vitro Study)
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Efficacy of Varnishes with: Bioactive Glass, Recaldent Technology and Silver Diamine Fluoride in Comparison with Sodium Fluoride on Tooth Surface Micro-hardness (an In Vitro Study)

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Publication Date
Sat Sep 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the efficacy of ultrasound in the diagnosis of cervical lymphadenopathy
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Background: Cervical lymph nodes are prone to involved by a number of pathologic processes. They are common sites for lymphoma, metastasis, and reactive enlargement in a number of conditions. Aims of the study:-Clinical evaluation of patients with cervical lymphadenopathy. Differentiation between benign and malignant lymph nodes by means of ultra sounds (US) and Correlate the US findings with cytological and/or histopathological findings of cervical lymph nodes. Subjects, Materials and Methods:-The present study was carried out over a period of 6 months and included 81 patients of different age groups presenting with cervical lymphadenopathy. Each patient was examined clinically, then comprehensive sonographic examination of the neck for

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Publication Date
Wed Mar 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
Anti-inflammatory effects of manuka honey on salivary cytokines (clinical study)
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Background: Manuka honey (MH) is a mono-floral honey derived from the Manuka tree (Leptospermum scoparium). MH is a highly recognized for its non-peroxide antibacterial activities, which are mostly related to its unique methylglyoxal content (MGO) in MH. The beneficial phytochemicals in MH is directly related to their favorable health effects, which include wound healing, anticancer, antioxidant, and anti-inflammatory properties. Aims: The purpose of this study was to evaluate the effect of MH on pro-inflammatory cytokines (IL-8 and TNF-α) in patients with gingivitis and compare it with chlorhexidine (CHX) and distilled water (DW). Materials and Methods: This study was a randomized, double blinded, and parallel clinical trial. Forty-fiv

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
The Value of Ultrasonography in The Diagnosis and Evaluation of Early Therapeutic Response of Cervical Tuberculous Lymphadenitis
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ABSTRACT Background: Tuberculosis is a worldwide infectious disease in spite of advancement in health care system. Tuberculous lymphadenitis is the most prevalent form of extra pulmonary tuberculosis with predilection of cervical lymph nodes. Objectives: To evaluate the reliability of grey scale ultrasonography together with color Doppler in the diagnosis of cervical tuberculous lymph adenitis and evaluation of early therapeutic response. Subjects and methods:From July 2015 to May 2016 in Al-Karama teaching hospital /Kut city- Wasit-Iraq, 25 patients (14 males and 11 females) with ages range from (6-50) years. Ultrasonography examination was done for all patients and grey scale criteria (distribution, size, shape, echogenicity, echogenic hi

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Publication Date
Fri Jul 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Performance Evaluation for Higher and Medium Leadership in Institutional Work Quality.
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Abstract:

This Research aims to define role of the system of evaluating the performance for higher leadership in determining the level of institutional work quality in the Ministry of Agriculture, by measuring system efficiency of evaluating the performance for higher leadership and its effect in institutional work quality, the searcher reached through the theoretical framing and involved studies to build default plan define the relation between Research variables formed from system of evaluating leadership performance as independent variable contains six subsidiary dimensions: (Polarization, evaluating the performance of personnel, training, motivation, se

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Publication Date
Wed Jun 01 2022
Journal Name
Resmilitaris
Evaluation mucin 1 polymorphism and expression with infertility in Iraqi females
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Scopus
Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
Root (GUM) and its derivatives between Lexical Sematics and Semantics Koranic
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As the word can fluctuate between central and peripheral dlalten it represents the first lexical meaning and the second represents the meaning that gain by the context in which it appear so this research came to show signs that can be acquired the root ( GUM ) and its derivatives from the contexts in which it is mentioned in the Koran as well as siqnificant Lexical if this research is divided on two first is eating Lexical semantics , the second handled connotations in the Koran was based on what the commentators and concemed with the meanings of the Koran and the owners Almagamat in astatement that the semantic .

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