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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 Sep 01 2022
Journal Name
Iop Conference Series: Earth And Environmental Science
Water Quality Status of Tigris River Using Index Analysis
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Abstract<p>This study investigates the effects of Al-Doura oil refinery effluent, in Baghdad city, on the water quality of the Tigris River using the Canadian Water Quality Index (CCME WQI) and Rivers Maintaining System (1967). Water samples were collected monthly from Tigris River at three stations, which are Al-Muthanna Bridge (upstream), Al-Doura Refinery (point source), and Al–Zafaraniya city (downstream) from October 2020 to April 2021. Fourteen water quality parameters were studied, namely pH (6.50-8.10), Water Temperature (WT) (5.00-27.00 °C), Electrical Conductivity (EC) (877.00-1192.00 μs/cm), Dissolved Oxygen (DO) (5.03-7.57 mg/L), Biological Oxygen demand (BOD) (0.53-2.23 mg/L), Total Dissolved S</p> ... Show More
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Publication Date
Tue Jun 02 2026
Journal Name
Natural And Engineering Sciences
Antibacterial Comparison of the Mango Seed Components by HPLC
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Crossref
Publication Date
Thu Jun 18 2026
Journal Name
Journal Of Administration And Economics
Using the Maximum Likelihood Method with a Suggested Weight to Estimate the Effect of Some Pollutants on the Tigris River- City of Kut
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The aim of this research is to use robust technique by trimming, as the analysis of maximum likelihood (ML) often fails in the case of outliers in the studied phenomenon. Where the (MLE) will lose its advantages because of the bad influence caused by the Outliers. In order to address this problem, new statistical methods have been developed so as not to be affected by the outliers. These methods have robustness or resistance. Therefore, maximum trimmed likelihood: (MTL) is a good alternative to achieve more results. Acceptability and analogies, but weights can be used to increase the efficiency of the resulting capacities and to increase the strength of the estimate using the maximum weighted trimmed likelihood (MWTL). In order to perform t

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Publication Date
Sun Aug 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
Measuring the impact of corporate governance mechanisms on social responsibility reports for a sample of Iraqi companies listed on the Iraq Stock Exchange
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The study aims to indicate the role of the mechanisms and principles of corporate governance in the activation of social responsibility reports, and increase disclosure, to achieve sustainability, legitimacy, and integrity of the business. Through the presentation of the conceptual framework for corporate governance and social responsibility, identify the key dimensions of social responsibility and the statement of the relationship between the mechanisms of governance and social responsibility reports in accordance with these dimensions. To prove the hypothesis research has selected a sample of listed companies in the Iraqi market for securities,

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Crossref
Publication Date
Sun Jun 30 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of strategic planning for electronic services to developing cash bank deposits: An Applied research for a sample of Iraqi private banks
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               The bank deposits is fuel banking activity and raw material products for the commercial bank and the basis of its activity and its lifetime So the bank, which seeks to continue the successful development of the volume of cash deposits has translated the work of the bank to meet the needs of different sectors by providing the necessary funding, and from this point of view was the research problem a lack of interest departments of banking services to commercial banks as a means for the development of electronic cash deposits have, and which represents the basis for the supplier commercial bank fund.

 

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Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Human Sport And Exercise - 2019 - Spring Conferences Of Sports Science
The effect of special force training on the development of biomechanical variables for running raising awareness during the performance on the jumping table
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Publication Date
Tue Oct 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
The impact of the RMB exchange rate on the value of Chinese exports For the period (1978-2017) using the Angel-Granger model
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In this research, we sought to identify the nature of the relationship between the exchange rate of the Chinese yuan and the value of Chinese exports, through the formulation of a standard model based on the model of common integration, and based on the data of the study and using the test "Angel-Granger" It reflects the relationship between the two research variables, through which the relationship between the RMB exchange rate and the value of Chinese exports was estimated during the period 1978-2017.

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Crossref
Publication Date
Tue Mar 30 2021
Journal Name
Journal Of Economics And Administrative Sciences
Analyzing indicators of the results of applying forecasting methods for production plans (A case study at the Diyala State Company for Electrical Industries)
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Economic organizations operate in a dynamic environment, which necessitates the use of quantitative techniques to make their decisions. Here, the role of forecasting production plans emerges. So, this study aims to the analysis of the results of applying forecasting methods to production plans for the past years, in the Diyala State Company for Electrical Industries.

The Diyala State Company for Electrical Industries was chosen as a field of research for its role in providing distinguished products as well as the development and growth of its products and quality, and because it produces many products, and the study period was limited to ten years, from 2010 to 2019. This study used the descriptive approa

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Crossref
Publication Date
Wed Jan 30 2019
Journal Name
Journal Of The College Of Education For Women
Taboo Words Vs. Social Deixis: A sociolinguistic Analysis of La Justice or The Cock that Crew: A Play from the Theatre of Ridiculous
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Linguistic taboos exist in most cultures. Tabooed words are generally being culturespecific
and relating to bodily functions or aspects of a culture that are sacred. Such words are
avoided, considered inappropriate and loaded with affective meaning and failing to adhere to.
Strict rules, often, governing their use and lead to punishment or public shame. These taboo
words can be used as a way of violating social deixis represented by four types of honorifics;
addressee, referent, bystander, and finally setting honorifics. This paper shows how these
taboo words are used in Kenneth Bernard's play La Justice or The Cock that Crew from the
theatre of the Ridiculous as means of violating social deixis in its four types. Th

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Publication Date
Fri Dec 12 2003
Journal Name
Iraqi Journal Of Laser
The Influence of Short Wavelength Laser on the Pupae Development of the Old World Screw- Worm Fly (OWSWF) Chrysomya bezziana Villeneuve (Diptera: Calliphoridae)
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The biological effects of pulsed N2-laser on the old world screw-worm fly, Chrysomya bezziana Villeneuve in the pupal stage were investigated. Different laser parameters were involved in this work. The old pupae of 1, 2, 3, 4 and 5 days were exposed to laser radiation during 10, 30 and 60 second with repetition rate 10, 20 and 30 pulse/second. The percent of normal adults emergence (female and male) was investigated. The results showed that the adults emergence was highly decreased as the repetition rate and exposure time increased when the pupae irradiated for 1, 2 and 3 days old as compared with 4 and 5 days. The results also indicated that the pupal period was significantly increased of irradiated pupae for 1, 2, 3 and 4 days old, whi

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