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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 Jun 07 2026
Journal Name
Accounting And Financial Sciences Journal
The Analyze of the Available Strategic Choices for External Borrowing (Futuristic Vision)
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يهدف البحث الى تحليل الخيارات الاستراتيجية للاقتراض الخارجي في العراق لاستشراف افضل الخيارات الاستراتيجية المستقبلية في مجال الاقتراض الخارجي في دائرة الدين العام في وزارة المالية ، وقد استخدم الباحث منهج دراسة الحالة وباستعمال اسلوب تحليل خوارزمية ال K-Means لتشخيص كفاءة الاقتراض الخارجي لعينة البحث البالغة (81) قرضا التي اقترضتها وزارة المالية للفترة 2007-2020 . ولقد كان الغرض الرئيسي للبحث المساهمة في تمكين وزا

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Publication Date
Wed May 15 2024
Journal Name
Chalcogenide Letters
Influence of annealing temperature on nano crystalline description for CuZnS thin films
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Copper Zinc Sulphide (Cu0.5Zn0.5S) alloy and thin films were fabricated in a vacuum. Nano crystallized (CZS) film with thick 450±20 nm was deposit at substrates glasses using thermal evaporation technique below ~ 2 × 10− 5 mbar vacuum to investigated the films structural, morphological and optical properties depended on annealing temperatures ( as-deposited, 423, 523 and 623) K for one hour. The influences annealed temperature on structurally besides morphologically characteristics on these films were investigated using XRD and AFM respectively. XRD confirms the formation a mixed hexagonal phase of CuS-ZnS in (102) direction with polycrystalline in nature having very fine crystallites size varying from (5.5-13.09) nm. AFM analys

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Publication Date
Tue Jun 01 2021
Journal Name
Journal Of The College Of Languages (jcl)
A Feminist Discourse Analysis of Writer's Gender Biases about Violence Against Women
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    The present study is concerned with the writer's ideologies towards violence against women. The study focuses on analyzing violence against women in English novel to see the extent the writers are being affected and influenced by their genders. It also focuses on showing to what extent the writer's ideologies are reflected in their works. Gender influences social groups ideologies; therefore, when a writer discusses an issue that concerns the other gender, they will be either subjective or objective depending on the degree of influence, i.e., gender has influenced their thoughts as well as behaviors. A single fact may be presented differently by different writers depending on the range of a

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Publication Date
Mon Jun 06 2022
Journal Name
Journal Of Experimental Agriculture International
Some Aspects of Life for Egg Parasite Pseudoligosita babylonica Viggiani (Hymenoptera: Trichogrammatidae)
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Due to the importance of egg parasitoids inthe natural and biological control of economically important insects, including egg parasitoid Pseudoligositaba bylonica Viggiani on dubas bug, the spread of the parasitoid and population distribution of parasitoid, In order to estimate the role of parasitoid as one of the biological factors in decreasing population density of dubas bug on date palm. Some aspects of the life of parasitoids were also studied, including the role of insect parasitoids in organizing the population of their families, geographical distribution and hosts range of genus Pseudoligosita, seasonal presence of parasitoid Pseudoligositaba bylonica Viggiani (Hymenoptera: Trichogrammatidae) , life studies and percentages

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Publication Date
Mon Jul 31 2023
Journal Name
Journal Of Biomimetics, Biomaterials And Biomedical Engineering
Investigating the Electrochemical Properties of Alkaloids Compound Derived from Catharanthus Roseus Extract
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The Catharanthus roseus plant was extracted and converted to nanoparticles in this work. The Soxhlet method was used to extract alkaloid compounds from the Catharanthus roseus plant and converted them to the nanoscale. Chitosan polymer was used as a linking material and converted to Chitosan nanoparticles (CSNPs). The extracted alkaloids were linked with Chitosan nanoparticles by maleic anhydride to get the final product (CSNPs-Linker-alkaloids). The pure Chitosan, Chitosan nanoparticles, and CSNPs-Linker-alkaloids were characterized by X-ray diffractometer, and Fourier Transform Infrared spectroscopy. X-ray results show that all samples have an orthorhombic structure with crystallite size in nanodimensions. FTIR spectra prove that

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Effect of High Temperatures on Biological Performance ofTrogoderma granarium (Everts) (Coleoptera: Dermestidae)
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The effect of three high temperatures for five exposure periods on the developments of larvae, pupae and adults of Trogoderma granarium (Everts) and their biological performance were investigated. The results revealed that the percent of mortality was increased as the temperature and the exposure period increased, e. g. exposing last instar larvae to 45°C for 6 hrs caused 100% death of this stage, while exposing adults (1-3) days old to the same temperature and exposure time resulted in that these adults did not able to survive more than 24 hrs.; in addition, the results showed that the ability of reproduction of adults was depended on the temperature, duration of exposure and the sex.

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Publication Date
Sun Feb 25 2024
Journal Name
Baghdad Science Journal
An Adaptive Harmony Search Part-of-Speech tagger for Square Hmong Corpus
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Data-driven models perform poorly on part-of-speech tagging problems with the square Hmong language, a low-resource corpus. This paper designs a weight evaluation function to reduce the influence of unknown words. It proposes an improved harmony search algorithm utilizing the roulette and local evaluation strategies for handling the square Hmong part-of-speech tagging problem. The experiment shows that the average accuracy of the proposed model is 6%, 8% more than HMM and BiLSTM-CRF models, respectively. Meanwhile, the average F1 of the proposed model is also 6%, 3% more than HMM and BiLSTM-CRF models, respectively.

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Publication Date
Tue Jul 01 2025
Journal Name
Research J. Pharm. And Tech
Fortification of Meat Burger with Protein Isolate Extracted from Local Pumpkin Seeds
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ABSTRACT: Protein isolate was achieved from local peeled non soaked pumpkins seeds by using petroleum ether with protein percentage of 53.15%. Protein isolate was used in manufacturing meat burger with two substitution10 and 20%. The shrinkage percentage for burger diameter was decreased from 25.5 to 16.6%, the sample with 10% substitution was distinguished in water holding capacity (WHC) which was 54.52%. Sensitive evaluation for these samples showed that the burger with 10% substitution was similar to the control.

Publication Date
Tue May 16 2023
Journal Name
Journal Of Engineering
EXPERIMENTAL INVESTIGATION OF INDIVIDUAL EVACUATED TUBE HEAT PIPE SOLAR WATER HEATING SYSTEMS
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lar water heating systems with heat pipes of three diameter groups of 16, 22 and 28.5 mm. The first and third groups had evaporator lengths of 1150, 1300 and 1550 mm. The second group had an additional length of 1800 mm. all heat pipes were of fixed condenser length of 200 mm. Ethanol at 50% fill charge ratio of the evaporator volume was used as the heat pipes working fluid. Each heat pipe condenser section was inserted in a storage tank and the evaporator section inserted into an evacuated glass tube of the Owens- Illinois type. The combined heat pipe and evacuated glass tube form an active solar collector of a unique design.
The resulting ten solar water heating systems were tested outdoors under the meteorological conditions of Bag

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Publication Date
Thu Jun 01 2023
Journal Name
Advances In Mechanical Engineering
3D-shape formation of blood vessels based on computer aided design system
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This paper proposes and tests a computerized approach for constructing a 3D model of blood vessels from angiogram images. The approach is divided into two steps, image features extraction and solid model formation. In the first step, image morphological operations and post-processing techniques are used for extracting geometrical entities from the angiogram image. These entities are the middle curve and outer edges of the blood vessel, which are then passed to a computer-aided graphical system for the second phase of processing. The system has embedded programming capabilities and pre-programmed libraries for automating a sequence of events that are exploited to create a solid model of the blood vessel. The gradient of the middle c

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