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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
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
Mon Aug 01 2022
Journal Name
Journal Of Engineering
Evaluation of Elaj Irrigation Project in Babil Governorate
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Climate change causes water shortage (water scarcity) in addition to the dams built by neighboring countries, which caused a lack of Iraq's water share. Therefore, evaluating the irrigation system requires considering its suitability, adequacy, and efficiency. Irrigation is considered adequate when it maintains water availability within the root zone, and if the amount to be added is determined, irrigation efficiency becomes possible by avoiding water loss. Babil Governorate is considered one of the agricultural governorates in the country that depends on its irrigation from Shatt Al-Hilla. The study area is the Elaj project. Three fields were selected for the project (B1, B2, and B3). These fields are lo

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Publication Date
Sat Apr 06 2024
Journal Name
Al- Anbar Medical Journal
Metastatic Ovarian Tumor from Incidental Renal Cell Carcinoma: A Case Report and Literature Review
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Publication Date
Fri Jul 07 2017
Journal Name
International Journal Of Science And Research (ijsr)
Automatic brain tumor segmentation from MRI Images using superpixels based split and Merge algorithm
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RA Ali, LK Abood, Int J Sci Res, 2017 - Cited by 2

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Publication Date
Mon Jul 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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Publication Date
Sat Jun 01 2024
Journal Name
Iaes International Journal Of Artificial Intelligence (ij-ai)
A novel fusion-based approach for the classification of packets in wireless body area networks
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This abstract focuses on the significance of wireless body area networks (WBANs) as a cutting-edge and self-governing technology, which has garnered substantial attention from researchers. The central challenge faced by WBANs revolves around upholding quality of service (QoS) within rapidly evolving sectors like healthcare. The intricate task of managing diverse traffic types with limited resources further compounds this challenge. Particularly in medical WBANs, the prioritization of vital data is crucial to ensure prompt delivery of critical information. Given the stringent requirements of these systems, any data loss or delays are untenable, necessitating the implementation of intelligent algorithms. These algorithms play a pivota

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Publication Date
Sun Oct 01 2023
Journal Name
Bulletin Of Electrical Engineering And Informatics
A novel data offloading scheme for QoS optimization in 5G based internet of medical things
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The internet of medical things (IoMT), which is expected the lead to the biggest technology in worldwide distribution. Using 5th generation (5G) transmission, market possibilities and hazards related to IoMT are improved and detected. This framework describes a strategy for proactively addressing worries and offering a forum to promote development, alter attitudes and maintain people's confidence in the broader healthcare system without compromising security. It is combined with a data offloading system to speed up the transmission of medical data and improved the quality of service (QoS). As a result of this development, we suggested the enriched energy efficient fuzzy (EEEF) data offloading technique to enhance the delivery of dat

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Publication Date
Sun Oct 01 2023
Journal Name
Bulletin Of Electrical Engineering And Informatics
A novel data offloading scheme for QoS optimization in 5G based internet of medical things
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The internet of medical things (IoMT), which is expected the lead to the biggest technology in worldwide distribution. Using 5th generation (5G) transmission, market possibilities and hazards related to IoMT are improved and detected. This framework describes a strategy for proactively addressing worries and offering a forum to promote development, alter attitudes and maintain people's confidence in the broader healthcare system without compromising security. It is combined with a data offloading system to speed up the transmission of medical data and improved the quality of service (QoS). As a result of this development, we suggested the enriched energy efficient fuzzy (EEEF) data offloading technique to enhance the delivery of dat

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