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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
Fri Nov 21 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Sonographic evaluation of masseter muscle thickness in bruxist and non-bruxist subjects
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Background: Masseter muscle is a jaw closing muscle of the mandible involved in Para functional habits; which include lip and cheek chewing, fingernail biting, and teeth clenching or bruxism which can be classified as awake or sleep bruxism. Patients with sleep bruxism are three to four times more likely to experience jaw pain and limitation of movement than people who do not experience sleep bruxism. The aim of this study is to measure the thickness of the masseter muscle in bruxist subjects and compare it with non-bruxist subjects by using sonography. Materials and Method: Forty Iraqi subjects with age ranged (20-40) divided into two groups according to the presence of bruxism. Clinical examination was made and masseter muscle thickness

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Publication Date
Mon Jul 01 2024
Journal Name
Indian Journal Of Clinical Biochemistry
Evaluation of Bone Turnover Markers in Patients with Acute and Chronic Leukemia
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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Sustained Release Sumatriptan Mucoadhesive Intranasal in-Situ Gel
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Sumatriptan(ST) is a selective agonist at serotonin 5-HTI receptors, as well as 5-HT1B/1D subtypes. It is effective for acute migraine attacks, but has a short half  life (about 2 hours) and low oral bioavailability (15%). The purpose of this study was to develop and optimize nasal mucoadhesive in-situ gel(IG) of ST to enhance nasal residence time for migraine management. Cold method was used to prepare different formulas of  ST nasal IG, using thermosensitive polymers (poloxamer 407  alone or with poloxamer 188) with a mucoadhesive polymer hyaluronic acid (HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, muc

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Publication Date
Sun Dec 31 2000
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Preparation of Tartaric Acid
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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Prediction of Hydraulic Flow Units for Jeribe Reservoir in Jambour Oil Field Applying Flow Zone Indicator Method
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The Jeribe reservoir in the Jambour Oil Field is a complex and heterogeneous carbonate reservoir characterized by a wide range of permeability variations. Due to limited availability of core plugs in most wells, it becomes crucial to establish correlations between cored wells and apply them to uncored wells for predicting permeability. In recent years, the Flow Zone Indicator (FZI) approach has gained significant applicability for predicting hydraulic flow units (HFUs) and identifying rock types within the reservoir units.

   This paper aims to develop a permeability model based on the principles of the Flow Zone Indicator. Analysis of core permeability versus core porosity plot and Reservoir Quality Index (RQI) - Normalized por

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Publication Date
Mon May 27 2019
Journal Name
Al-khwarizmi Engineering Journal
Prediction of Process Parameters That Affecting on Surface Roughness in Multi-Point Forming Process Using ANOVA Algorithm
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Multipoint forming process is an engineering concept which means that the working surface of the punch and die is produced as hemispherical ends of individual active elements (called pins), where each pin can be independently, vertically displaced using a geometrically reconfigurable die. Several different products can be made without changing tools saved precious production time. Also, the manufacturing of very expensive rigid dies is reduced, and a lot of expenses are saved. But the most important aspects of using such types of equipment are the flexibility of the tooling. This paper presents an experimental investigation of the effect of three main parameters which are blank holder, rubber thickness and forming speed th

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Crossref
Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Prediction of Hydraulic Flow Units for Jeribe Reservoir in Jambour Oil Field Applying Flow Zone Indicator Method
...Show More Authors

The Jeribe reservoir in the Jambour Oil Field is a complex and heterogeneous carbonate reservoir characterized by a wide range of permeability variations. Due to limited availability of core plugs in most wells, it becomes crucial to establish correlations between cored wells and apply them to uncored wells for predicting permeability. In recent years, the Flow Zone Indicator (FZI) approach has gained significant applicability for predicting hydraulic flow units (HFUs) and identifying rock types within the reservoir units.    This paper aims to develop a permeability model based on the principles of the Flow Zone Indicator. Analysis of core permeability versus core porosity plot and Reservoir Quality Index (RQI) - Normalized poros

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Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Use of Coliphages as an indicators of enteroviruses and faecal pollution in Water
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In spite of increasing clinical cases which caused by enteroviruses transferred by water and no documents about entericviruses in the Iraqi water standards. The use of coliphages as an indicator of enteroviruses and fecal pollution were suggested two procedures were applied . The first is Two-Step Enrichment Method and the second is Single Agar Layer Method. Both methods gives good results in Identification of coliphages through testing fifty different water samples (Tap water, Surface water and Bottled water) the study shows the presence of coliphages in fourteen samples.

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Publication Date
Thu May 31 2012
Journal Name
Al-khwarizmi Engineering Journal
Channel Estimation and Prediction Based Adaptive Wireless Communication Systems
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Wireless channels are typically much more noisy than wired links and subjected to fading due to multipath  propagation which result in ISI and hence high error rate. Adaptive modulation is a powerful technique to improve the tradeoff between spectral efficiency and Bit Error Rate (BER). In order to adjust the transmission rate, channel state information (CSI) is required at the transmitter side.

In this paper the performance enhancement of using linear prediction along with channel estimation to track the channel variations and adaptive modulation were examined. The simulation results shows that the channel estimation is sufficient for low Doppler frequency shifts (<30 Hz), while channel prediction is much more suited at

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Publication Date
Fri Nov 21 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of orthodontic tooth movement on salivary levels of Interleukin-1beta, Tumor Necrosis Factor-alpha, and C- reactive protein
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Background: Orthodontic force is considered to stimulate cells in the periodontium to release many mediators such as cytokines which play a responsible role for periodontal and alveolar bone remodeling, bone resorption and new bone deposition. Aim of this study was carried out to estimate changes of the (interleukin-one beta, tumor necrosis factor – alpha and C-reactive protein) levels in unstimulated whole saliva during the leveling stage of orthodontic tooth movement. Materials and methods: The sample consisted of thirty adult patients (12 males and 18 females) with ages ranges (19-23) years. Each sample had Class I and Class II malocclusion dental classification and required bilateral extraction of their maxillary first premolars, und

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