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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
Journal Of Economics And Administrative Sciences
Petroleum Derivatives in Iraq The phenomenon of Renewable or Passing crisis
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     Iraq economy suffered, nor , still many difficulties and problems , including oil derivatives crisis that emerged in 2004 and was the most prominent features of the inability of local production to meet the needs of the increasing growth of consumption, the crisis has cast a shadow on the growth of national in general, and citizen living in particular. Therefore, the real test of crisis and challenge to the capacity of government agencies to manage the crisis and control and reduce its harmful effects, which disappear in a region or sector, even begin to appear in another, given the multiplicity and complexity of third-party solution for remedying the negative consequences of deliberate.

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Publication Date
Sun Feb 02 2025
Journal Name
Journal Of Baghdad College Of Dentistry
An Extrafollicular Cystic Adenomatoid Odontogenic Tumor of the Mandible Associated with Clear Cell Calcifying Epithelial Odontogenic Tumor: A Rare Case Report
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Background: The adenomatoid odontogenic tumor is a relatively rare benign epithelial odontogenic tumor. It contains both epithelial and mesenchymal components. Few cases presented as an extrafollicular lesion or involve the mandible or associated with other odontogenic lesions. This paper represents a rare case of an extrafollicular AOT. Case presentation: A 24-year-old female had a painless swelling on the right side of the lower jaw since one-month duration. Intraorally there was a well defined fluctuant-blue swelling in the right alveolar premolar region measuring 1×2 cm obliterating the right lower buccal vestibule. Grade II mobility in the vital 44 and 45 teeth were observed. Panoramic radiographs showed a well-defined pear shaped

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Publication Date
Thu May 04 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
The Effect of Electromagnetic Current in the Plantlet in vitro in Cucumis sativus L.
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Seeds of three American species of cucumber:-Lot number (EM285) signed as number 1,
To CAEEN F1 signed as number 2 ,and Hybird Super Green F1 signed as number 3, were
exposed to two kinds of physical effects .They were given :- 4 frequencies of the electric
current (0,1,2and 2.5) Am for five minutes using electro- magnetic generator .Then the three
species exposed to Ultra-Violet (UV)wave for four periods (0,30,60 and 90)sec. respectively
at 254 nm using Hood light .After exposure time the seeds were planted in sterlized
media(MS) with Benzyladenine (BA)and left in the incubator for2-3 weeks .Then ,plantlets of
the three species were taken to study the root system ,shoot system ,dry and wet weight for
them

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Publication Date
Sun Dec 02 2012
Journal Name
دراسات عربية في التربية وعلم النفس
The effectiveness of environmental enrichment activities in the achievement of chemistry and environmental awareness for fifth-grade science students
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Publication Date
Wed Aug 30 2023
Journal Name
Al-kindy College Medical Journal
Pancreatic Stone Protein/ regenerating Protein (PSP/reg) as a Biochemical Marker for prediction of Microvascular Complications of Type 2 Diabetes Mellitus
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Background: Type 2 diabetes mellitus (T2DM) characterized by insulin resistance (IR) and progressive decline in functional beta (β) cell mass partially due to increased β cell apoptosis rate. Pancreatic stone protein /regenerating protein (PSP/reg) is produced mainly by the pancreas and elevated drastically during pancreatic disorder. Beta cells are experiencing apoptosis that stimulate the expression of PSP/reg gene in surviving neighboring cells, and that PSP/reg protein is subsequently secreted from these cells which could play a role in their regeneration.

Objectives: To analyze serum levels of PSP/reg protein in T2DM patients and evaluate its correlation with the microvasc

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Publication Date
Wed Jan 13 2021
Journal Name
Iraqi Journal Of Science
The Use of CUSB Model to Simplify Business Plans the Case of the Promotion of A Heritage Site in Morocco
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In today‟s fierce competitive world, entrepreneurship has taken an upswing because business owners are facing a technological challenge in which uniqueness and particularity are key elements to detour rivals. In this essence, entrepreneurs have to go by not only developing business plans but also a deep analysis of their environment.
Business plans for entrepreneurs can take different models depending on the party that will evaluate its elements based on its requirements. However, there exists a basic format that most entrepreneurs follow. Because of time constraints, business owners are urging its usefulness and so are the investors. Business plans are all about nailing down the business idea into writing and analysis, while th

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Publication Date
Fri Dec 24 2021
Journal Name
Iraqi Journal Of Science
The Optimum Site Selection for Solar Energy Farms using AHP in GIS Environment, A Case Study of Iraq
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    Recently, renewable energy (RE), such as solar energy, sources have proven their importance as an alternative source of fuel. The utilizing of solar energy can contribute to move the world towards relying on clean energy to curb global warming. However, the placement of solar farms is a major priority for planners as it is a critical factor in the succession energy project. This study combines one of the multi-criteria decision-making techniques Analytic Hierarchy Process (AHP) and Geographic Information System (GIS) to assess the suitability of land for establishing solar farms in Iraq. Numerous climatic, geomorphological, economic, and environmental criteria and some exclusionary constraints have been adopted in mode

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Publication Date
Sat Feb 26 2022
Journal Name
Iraqi Journal Of Science
Effects of Psidium Guajava Leaves Extract on the Viability of Echinococcus Granulosus Protoscolices in Vitro and in Vivo
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     Echinococcosis is a common parasitic disease in humans and ruminants; it is considered as a health and economic problem in most parts of the world. The present study aims to evaluate the in vitro and in vivo scolicidal effects of Psidium guajava extracts on the protoscolices from hydatid cysts of Echinococcus granulosus. Protoscolices were aseptically aspirated from the livers of naturally infected sheep. Various concentrations of the extract were used for 6-48hrs. Eosin staining (0.1%) was used to determine the viability of protoscolices. The findings showed that the extract at the concentrations of 100 mg/ml killed 100% protoscolices after 48 hrs. However, the concentrations

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Publication Date
Sun Apr 07 2013
Journal Name
Journal Of Educational And Psychological Researches
Effectiveness of enrichment activities through using software program for second graders in Conversation article
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Today we are witnessing huge scientific and technical progress so we need more skills and methods of thinking that needs to be acquired by the teacher, as the importance of computers in education  there are  many teachers  suffering  of the difficulty in teaching for pupils . researchers tried to  find a good suitable way with the technological  interests for now which represent by  computer design software and the introduction of enrichment activities in the curriculum because it is one of a contemporary trends for the development of the Arabic language with various levels of education and knowing if this program has negative or positive impact.

So&nbsp

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Publication Date
Sun Dec 30 2001
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Regeneration of SLFO_Nitro Acid Mixture in Continuous Mode Operation
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