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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 Jan 30 2014
Journal Name
Al-kindy College Medical Journal
Relationship between Very Low Birth Weight Neonates and increased Neonatal mortality for age 0 to 7 days
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B aa cc kk gg r oo uu nn dd : Very low birth weight (VLBW) neonates constitute approximately 4–7 percent of all live births and their mortality is very high. O bb j ee cc t i vv ee: to find out if there is a relationship between Very Low Birth Weight Neonates and increased neonatal mortality for age 0 to 7 days. M ee t hh oo dd ss A retrospective study of VLBW neonates admitted to NICU at Ibn Al- Baladi Pediatrics and Maternity hospital over one year (2012)were studied, study period was from April till August 2013. Exclusion criteria were: (1) neonates weighing less than 700 g and with gestational age less than 24 weeks (abortion) (2) death in the delivery room (3) neonates weighing more than 1500 g. (4) Postnatal age more than 7 days.

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Publication Date
Thu May 05 2022
Journal Name
Karbala International Journal Of Modern Science
Nigella sativa Methanol Extract Inhibits PC-3 Cell Line Colonization, Induced Apoptosis, and Modulated LC3-based Autophagy
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Nigella sativa has various pharmacological properties and has been used throughout history for a variety of reasons. However, there is limited data about the effects of N. sativa (NS) on human cancer cells. This study aimed at observing the roles of methanolic extract of N. sativa on apoptosis and autophagy pathway in the Human PC3 (prostate cancer) cell line. The cell viability was checked by MTT assay. Clonogenic assay was performed to demonstrate clonogenicity and Western blot was used to check caspase-3, TIGAR, p53, and LC3 protein expression. The results demonstrated that PC3 cell proliferation was inhibited, caspase-3 and p53 protein expression was induced, and LC3 protein expression was modulated. The clonogenic assay showed that PC3

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Publication Date
Thu Dec 31 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Financial analysis indicators and their impact on investment decision-making: for the national insurance company (applied research)
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The financial analysis of the published financial statements is the means that enables businessmen, financial institutions, financial analysts and others to conduct their studies and conclusions to obtain information that helps them in the decision-making process, including decisions related to investment. National in making the decision on the investment activity, for the period from 2012 to 2018, through the information provided by the annual financial statements, by selecting a set of indicators provided by the financial statements, namely (liquidity ratio, activity percentage, profitability ratios) to measure the extent of this ability Indicators in determining their role in making an investment decision.

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Publication Date
Wed Mar 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Estimation Pore and Fracture Pressure Based on Log Data; Case Study: Mishrif Formation/Buzurgan Oilfield at Iraq
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Prediction of the formation of pore and fracture pressure before constructing a drilling wells program are a crucial since it helps to prevent several drilling operations issues including lost circulation, kick, pipe sticking, blowout, and other issues. IP (Interactive Petrophysics) software is used to calculate and measure pore and fracture pressure. Eaton method, Matthews and Kelly, Modified Eaton, and Barker and Wood equations are used to calculate fracture pressure, whereas only Eaton method is used to measure pore pressure. These approaches are based on log data obtained from six wells, three from the north dome; BUCN-52, BUCN-51, BUCN-43 and the other from the south dome; BUCS-49, BUCS-48, BUCS-47. Along with the overburden pressur

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Publication Date
Tue Jan 16 2018
Journal Name
Design And Manufacture An Automatic Knife For Date Palm Tree Frond Cutting Operates By Frequency Theory Cutting‏ Mra Abdulrazak A. Jasim‏
Design and manufacture an automatic knife for date palm tree frond cutting Operates by frequency theory Cutting‏
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Publication Date
Thu Jan 30 2020
Journal Name
Journal Of Engineering
  Positional Accuracy Assessment for Updating Authoritative Geospatial Datasets Based on Open Source Data and Remotely Sensed Images
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OpenStreetMap (OSM) represents the most common example of online volunteered mapping applications. Most of these platforms are open source spatial data collected by non-experts volunteers using different data collection methods. OSM project aims to provide a free digital map for all the world. The heterogeneity in data collection methods made OSM project databases accuracy is unreliable and must be dealt with caution for any engineering application. This study aims to assess the horizontal positional accuracy of three spatial data sources are OSM road network database, high-resolution Satellite Image (SI), and high-resolution Aerial Photo (AP) of Baghdad city with respect to an analogue formal road network dataset obtain

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Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
Solving Whitham-Broer-Kaup-Like Equations Numerically by using Hybrid Differential Transform Method and Finite Differences Method
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This paper aims to propose a hybrid approach of two powerful methods, namely the differential transform and finite difference methods, to obtain the solution of the coupled Whitham-Broer-Kaup-Like equations which arises in shallow-water wave theory. The capability of the method to such problems is verified by taking different parameters and initial conditions. The numerical simulations are depicted in 2D and 3D graphs. It is shown that the used approach returns accurate solutions for this type of problems in comparison with the analytic ones.

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Publication Date
Thu Dec 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
Dynamic algorithm (DRBLTS) and potentially weighted (WBP) to estimate hippocampal regression parameters using a techniqueBootstrap (comparative study)
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Bootstrap is one of an important re-sampling technique which has given the attention of  researches recently. The presence of outliers in the original data set may cause serious problem to the classical bootstrap when the percentage of outliers are higher than the original one. Many methods are proposed to overcome this problem such  Dynamic Robust Bootstrap for LTS (DRBLTS) and Weighted Bootstrap with Probability (WBP). This paper try to show the accuracy of parameters estimation by comparison the results of both methods. The bias , MSE and RMSE are considered. The criterion of the accuracy is based on the RMSE value since the method that provide us RMSE value smaller than other is con

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Publication Date
Wed Mar 01 2023
Journal Name
Iaes International Journal Of Artificial Intelligence (ij-ai)
Design and implementation monitoring robotic system based on you only look once model using deep learning technique
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<span lang="EN-US">The need for robotics systems has become an urgent necessity in various fields, especially in video surveillance and live broadcasting systems. The main goal of this work is to design and implement a rover robotic monitoring system based on raspberry pi 4 model B to control this overall system and display a live video by using a webcam (USB camera) as well as using you only look once algorithm-version five (YOLOv5) to detect, recognize and display objects in real-time. This deep learning algorithm is highly accurate and fast and is implemented by Python, OpenCV, PyTorch codes and the Context Object Detection Task (COCO) 2020 dataset. This robot can move in all directions and in different places especially in

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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Emulsion Liquid Membrane for Pesticides Removal from Aqueous Solution: Emulsion Stability, Extraction Efficiency and Mass Transfer Studies
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The current study investigated the stability and the extraction efficiency of emulsion liquid membrane (ELM) for Abamectin pesticide removal from aqueous solution. The stability was investigated in terms of droplet emulsion size distribution and emulsion breakage percent. The proposed ELM included a mixture of corn oil and kerosene (1:1) as a diluent, Span 80 (sorbitan monooleate) as a surfactant and hydrochloric acid (HCl) as a stripping agent without utilizing a carrier agent. Parameters such as homogenizer speed, surfactant concentration, emulsification time and internal to organic volume ratio (I/O) were evaluated. Results show that the lower droplet size of 0.9 µm and higher stable emulsion in terms of breakage percent of 1.12 % we

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