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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
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Evaluation of Pedestrians Walking Speeds in Baghdad City
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This research examines the factors which influence pedestrian's walking speed in Baghdad. the variations in walking speed of pedestrians are related to pedestrian characteristics such as gender, age group, and clothing traditions. Using the established methodology, the counts of pedestrians were performed using manual and video counting. The case study was performed in two streets located in a highly crowded commercial zone at the city center of Baghdad: Al-Karada Dakhel and Al- Sina’a Street. Data were subjected to statistical analysis using IBM SPSS Statistics 19 software. It has been found that Iraqi pedestrians walk slower than other pedestrians in the developed countries or in the region with minimum walking speed of 29.85 m/min.

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Publication Date
Sat Sep 01 2012
Journal Name
2012 8th International Conference On Wireless Communications, Networking And Mobile Computing
Performance Evaluation of Location Management in GSM Networks
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Publication Date
Thu Sep 01 2016
Journal Name
Journal Of Engineering
Evaluation of Maintenance Management in Iraqi Governmental Buildings
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Impact of buildings in Iraq and other countries on the environment is obvious; this problem began to take scientific and humanitarian dimensions in order to reduce and eliminate this problem. This impact can be seen through the energy, water and raw materials consumed for the establishment, operation and maintenance of these buildings, as well as the emissions of hazardous gases and generations of solid wastes.

This work was conducted to assess the current maintenance managerial practice for the governmental buildings to stand on the main obstacle and extrapolation of measures by means of interviews with experts to determine the effective factors and closed questionnaire to state the features and the need for new

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Publication Date
Sat Mar 01 2008
Journal Name
Al-khwarizmi Engineering Journal
Evaluation of Hydrated Lime Filler in Asphalt Mixtures
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Mineral filler is one of important  materials and affecting on properties and quality of asphalt mixtures .There are different types of mineral filler depended on cost and quality , the matter encourages us to achieve this study to evaluate hydrated lime filler effects on properties of asphalt mixes related with strength and durability. Conventional asphaltic concrete mixtures with Portland cement and soft sandstone fillers and mixtures modified with hydrated lime were evaluated for their fundamental engineering properties as defined by Marshall properties , index of retained strength , indirect tensile strength , permanent deformation characteristics , and fatigue resistance .A typical dense graded mixture employed in construction

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Publication Date
Sun Aug 31 2025
Journal Name
Journal Of Science In Medicine And Life
Serum Endothelial Specific Molecule 1(EMS 1) and Uric Acid Levels in Severe Preeclampsia
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Publication Date
Tue Dec 04 2018
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EVALUATION OF IMPACT OF MARKETING POLICY IN Al-FURAT GENERAL COMPANY FOR CHEMICAL INDUSTRIES AND PESTICIDES: EVALUATION OF IMPACT OF MARKETING POLICY IN Al-FURAT GENERAL COMPANY FOR CHEMICAL INDUSTRIES AND PESTICIDES
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Marketing is one of the most important pillars on which most industrial and commercial sectors depend on evaluating their performance, improving their financial position, development and economic growth. The presence of effective marketing activities in any industrial or commercial organization (which works to meet the requirements of customers in order to ensure the integration of trading and handling rings with consumers and to ensure the growth of the marketing process regularly and not to retreat) effectively contributes to maintaining the company's position between its competitors and its customers. It is necessary to have these marketing activities in order to meet the requirements of the organization on the one hand and to

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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
Evaluation of Lands in Yusufiya County -study in the soil geographic
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This study has contributed to identify convenience of the land Usifiya of Mahmudiya district baghdad province for the cultivation of sensitive and salt resisting crops and growing pasture .The nine pedons (tracks) of the study have spread over three transects to cover the whole area the north, middle and south .
Depending on Visual Space tupe (TM) for 2007 which is super classified, samples are distributed on all classes of land cover
It is detected the presence of nine series soils namely
MM5- MW96- DM 115 for 1st transect
MF12- DM46 - DM96 for 2nd transect
DM56- DF56 - MW5 for 3rd transect
Soils are classified to the level of sub great group according to (soil Survey Staff) to :
*Typic Torri Fluvents , Typic Haplos

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Publication Date
Thu Dec 31 2015
Journal Name
Wuhan University Journal Of Natural Sciences
Prolactin is a Novel Biochemical Marker in Sera of Iraqi Type-2 Diabetic Women With Metabolic Syndrome in Baghdad.
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Abstract Metabolic syndrome (MS) is a group of clinical and biological abnormalities included risk of insulin resistance , disorders in glucose metabolism , abdominal obesity and abnormal lipid profile these features confer a greater risk of cardiovascular diseases . Anyway, the co-occurrence of diabetes mellitus and metabolic syndrome potentiates the cardiovascular risk associated with each of the two conditions. The present study aimed to determine a relationship between prolactin level in type -2- diabetic Iraqi women and metabolic syndrome, as well to find a relationship between prolactin level and other studied biochemical markers. seventy menopausal diabetic women with metabolic syndrome with age in range (45-50) years were enrolled i

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Publication Date
Mon Jan 01 2024
Journal Name
Aip Conference Proceedings
Investigation in vitro the effect of X-rays, gamma rays and beta particles on the physical and structural characteristics of human teeth
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Publication Date
Fri Feb 27 2026
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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