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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
Wed Dec 01 2010
Journal Name
Al-khwarizmi Engineering Journal
The Biosorption of Cr (VI) From Aqueous Solution Using Date Palm Fibers (Leef)
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The ability of Cr (VI) removal from aqueous solution using date palm fibers (leef) was investigated .The effects of pH, contact time, sorbets concentration and initial  metal ions concentration on the biosorption were investigated.

The residual concentration of Cr (VI) in solution was determined colorimetrically using spectrophotometer at wave length 540 nm .The biosorption was pH-dependent, the optimum pH was 7 and adsorption isotherms obtained fitted well with Langmuir isotherms .The Langmuir equation obtained was Ce/Cs = 79.99 Ce-77.39, the correlation factor was 0.908.These results indicate that date palm fibers (leef) has a potential effect for the uptake of Cr (VI) from industrial waste water.

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Publication Date
Sat Dec 14 2019
Journal Name
International Journal On Emerging Technologies
Utilizing an Artificial Neural Network Model to Predict Bearing Capacity of Stone Columns
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ABSTRACT: Ultimate bearing capacity of soft ground reinforced with stone column was recently predicted using various artificial intelligence technologies such as artificial neural network because of all the advantages that they can offer in minimizing time, effort and cost. As well as, most of applied theories or predicted formulas deduced analytically from previous studies were feasible only for a particular testing environment and do not match other field or laboratory datasets. However, the performance of such techniques depends largely on input parameters that really affect the target output and missing of any parameter can lead to inaccurate results and give a false indicator. In the current study, data were collected from previous rel

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Scopus
Publication Date
Sun Jul 30 2023
Journal Name
American Journal Of Environmental Economics
Impact of Brand Capital on the Stock Price Crash Risk, an Empirical Study
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The factors influencing the financial market are rapidly becoming more complex. The impact of non-financial factors on the performance of a company’s common stock can increase in ways that were not previously expected. This study investigated how brand capital affects the risk of stock prices in Iraqi private banks listed on the Iraq Stock Exchange failing by identifying the likelihood of a crash caused by a negative deviation in the distribution of returns on ordinary shares. As a result, the current study’s concept is to review an analytical knowledge framework of the nature of that relationship, its changes, and its impact on the pricing of ordinary shares of the banks of the researched sector for the years 2009 to 2017, as w

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Theoretical Studies of Sum Optical Properties for InAs (001) by Surface Differential Reflectivity
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The real and imaginary part of complex dielectric constant for InAs(001) by adsorption of oxsagen atoms has been calculated, using numerical analysis method (non-linear least square fitting). As a result a mathematical model built-up and the final result show a fairly good agreement with other genuine published works.

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Publication Date
Sun Mar 15 2020
Journal Name
Al-academy
The Image of Woman by the Artist Jaber Alwan: احلام عبد الستار شنين
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The woman represents an existential dualism with the man along history. This existence has been manifested through the history of Art starting from the arts of the old civilizations until modernism. It must be said that the history of Art refers to her presence as an extension for this history in the oriental arts, and the Arab countries including Iraq.  The woman has varying outputs in terms of the content of her presence and the style of presentation. In her characterizations: maternity, fertility, femininity and others. The Iraqi artists adopted these fields among them the artist Jaber Alwan who formulated his style of presentation and its units depending on the feminine presence and his experience in her formal and stylistic fie

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Crossref
Publication Date
Wed Feb 01 2023
Journal Name
International Journal Of Electrical And Computer Engineering
Classification of COVID-19 from CT chest images using Convolutional Wavelet Neural Network
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<p>Analyzing X-rays and computed tomography-scan (CT scan) images using a convolutional neural network (CNN) method is a very interesting subject, especially after coronavirus disease 2019 (COVID-19) pandemic. In this paper, a study is made on 423 patients’ CT scan images from Al-Kadhimiya (Madenat Al Emammain Al Kadhmain) hospital in Baghdad, Iraq, to diagnose if they have COVID or not using CNN. The total data being tested has 15000 CT-scan images chosen in a specific way to give a correct diagnosis. The activation function used in this research is the wavelet function, which differs from CNN activation functions. The convolutional wavelet neural network (CWNN) model proposed in this paper is compared with regular convol

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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
Remediation of Groundwater Contaminated with Copper Ions by Waste Foundry Sand Permeable Barrier
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The permeable reactive barrier (PRB) is one of the promising innovative in situ groundwater remediation technologies, in removing of copper from a contaminated shallow aquifer. The 1:1- mixture of waste foundry sand (WFS) and Kerbala’s sand (KS) was used for PRB. The WFS was represented the reactivity material while KS used to increase the permeability of PRB only. However, Fourier-transform infrared (FTIR) analysis proved that the carboxylic and alkyl halides groups are responsible for the sorption of copper onto WFS. Batch tests have been performed to characterize the equilibrium sorption properties of the (WFS+KS) mix in copper- containing aqueous
solutions. The sorption data for Cu+2 ions, obtained by batch experiments, have be

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Crossref
Publication Date
Tue Sep 01 2020
Journal Name
Journal Of Engineering
Buckling Behavior of Aluminum Alloy Thin-Walled Beam with Holes under Compression Loading
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Thin-walled members are increasingly used in structural applications, especially in light structures like in constructions and aircraft structures because of their high strength-to-weight ratio. Perforations are often made on these structures for reducing weight and to facilitate the services and maintenance works like in aircraft wing ribs. This type of structures suffers from buckling phenomena due to its dimensions, and this suffering increases with the presence of holes in it. This study investigated experimentally and numerically the buckling behavior of aluminum alloy 6061-O thin-walled lipped channel beam with specific holes subjected to compression load. A nonlinear finite elements analysis was used to obtain the

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Publication Date
Mon Jan 01 2024
Journal Name
2nd International Conference For Engineering Sciences And Information Technology (esit 2022): Esit2022 Conference Proceedings
Calculating land surface temperature of South Baghdad by the using Landsat 8 images
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Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
Antifungal Potential of Cladosporium sp. (Endophytic fungi) Associated with Olea europaea L. Leaves
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In the leaves of Olea europaea L. Olive trees an endophytic fungus was discovered. Cladosporium sp. was identified to be the fungus based on its morphological characteristics and nuclear ribosomal DNA ITS sequence analysis and was registered in NCBI as the Cladosporium genus has been registered under the number (0P939922.1) The species was not specified, and it was considered of unknown species after comparing it to global isolates. In comparison to olive leaf extract, Cladosporium sp. including total flavonoid, total phenolic, total terpenoid, and total saponins, Which were 121.9%, 198.1%, 89.13%, and 29.87 % respectively compared to its content in olive leaf extract, which was 61.54 %, 67.88 % , 17.1

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