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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 Aug 13 2017
Journal Name
Iraqi Journal Of Agricultural Sciences
EFFECT OF SUPPLEMENTING DIFFERENT LEVELS OF CONJUGATED LINOLEIC ACID (CLA) TO THE DIET ON PRODUCTIVE PERFORMANCE OF BROILER CHICKEN
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This study was carried out at Poultry Research Station, State Board of Agricultural Research, Ministry of Agriculture for the period from 27 September 2014 to 9 November 2014 to evaluate the Supplementation of different levels of Conjugated Linoleic Acid (CLA) on productive performance of broiler. Four hundred eighty chicks (Ross-308),one day old were randomly distributed to four dietary treatments for 42 days of age with 3 replicates/vtreatment (40 bird/replicate). Experimental treatments were as follow; T1 (Control diet) without supplement, while the treatment T2,T3 and T4  were Supplemented with 1, 1.5, 2 g CLA /kg diet  respectively. The results showed significant (P ≤ 0.05) increased in mean of body weight, weight gain, ave

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Publication Date
Thu Jul 01 1999
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
Grain size and sorting as indicators of depositional environment of ghar formation (late lower Miocene), Iraq
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Char formation is subdivided into three lithological types according to the percentage of detrital quartz and calcite (micrite and sparite), through the petrographic study of 13 thin sections collected from a section at Wadi Al-Ratgha (west of Al-Qaim, Iraq Western Desert). The three rock units are: Limy sandstone, limestone and sandy limestone. Depending on the mean gain size of detrital quartz and degree of sorting and the type of matrix, Ghar Formation can be classified in to three types, i. e. off-shore sediments with low energy environment, near shore sediments with high energy environment and mixed sediments with transitional energy environment. This is due to local transgression and regression of sea level at late lower Miocene du

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Publication Date
Sun Jul 23 2023
Journal Name
University Of Samarra
Synthesis, spectral characterization and thermal ‎study of complexes of ions of some metallic ‎elements with new cyclic ligands
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The purpose of my thesis is to prepare four new ligands (L1-L4) that have been ‎used to prepare a series of metal complexes by reacting them with metal ions:‎ ‎ M=(Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II) ‎ ‎ Where succinyl chloride was used as a raw material for the preparation of ‎bi-dented ligands (L1-L4) by reacting it with potassium thiocyanate as a first ‎step and then reacting with (2-aminobenzothiazole, Benzylamine, 4-‎aminoantipyrine, Sulfamethoxazole) respectively as a second step with the use ‎of dry acetone as a solvent, the chemical formula of the four ligands prepared in ‎succession:‎ N1,N4-bis(benzo[d]thiazol-2-ylcarbamothioyl)succinamide (L1)‎ N1,N4-bis(benzylcarbamothioyl)succinami

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Publication Date
Fri Jun 28 2019
Journal Name
Journal Of The College Of Education For Women
Creative Formation in the Poetry of Thafer Bin Qasim Al-Haddad (529 A.H) (Creative Ingenuity as Model): خلود هاشم جوحي الوائلي
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Through research and research in the creative composition in the poetry of Zafer-Alhaddad it turned out to be superior in its systems, especially that he chose a linguistic and verbal texture accompanied by a cultural dictionary full of creativity and beauty helped this culture arrangement reflects the poetically wonderful and beautiful custom led to the harmony of colors and bodies painted by the poet brush the creative artist evaluates the metaphorical and metaphorical relations that would explain the poets idea, most of which were inspired by the wonderful spirit of nature, its beautiful landscapes and bright colors, especially that we do not forget the beautiful colors and the aesthetic touch that created a fascinating musical intera

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Publication Date
Wed Mar 04 2026
Journal Name
Al–bahith Al–a'alami
Objectivity of the Liaison in the Iraqi Media Institutions (Al Mada, Azzaman, Al-Sumaria, Aletejah Instituations & Satalite Channels as a Model)
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Objectivity is the common denominator between the qualities and elements of a news story that is described as the mother of journalistic arts. When there is doubt about the authenticity of the information contained in the press, whether readable, audible or visual, it means that there is an imbalance in objectivity. When, furthermore, there is an incorrect and intentional use of words in order to influence readers, it means to move away from objectivity as a necessary element in the success of the media institution; and the success of its editorial material.

But the objective interpretation may take several dimensions to the liaison. For the purpose of grasping the interpretation of objectivity among those liaisons working in the

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Publication Date
Thu Nov 30 2023
Journal Name
Research Journal Of Pharmacy And Technology
Preparation and Evaluation of Aceclofenac Solid Dispersion by Fusion Technique and Effervescent Assisted Fusion Technique: Comparative Study
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Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction

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Publication Date
Mon Mar 02 2020
Journal Name
Journal Of Applied Research In Higher Education
Proposal of a guide for talent evaluation and management based on a qualitative and three-staged approach
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Purpose

The key objective of the study is to understand the best processes that are currently used in managing talent in Australian higher education (AHE) and design a quantitative measurement of talent management processes (TMPs) for the higher education (HE) sector.

Design/methodology/approach

The three qualitative multi-method studies that are commonly used in empirical studies, namely, brainstorming, focus group discussions and semi-structured individual interviews were considered. Twenty-three individuals from six Australian universities parti

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Publication Date
Wed Dec 20 2023
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Systemic Melatonin Supplementation as an Adjunct to Non-Surgical Periodontal Treatment in Obese Patients with Periodontitis
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Background: Obesity is considered an important risk factor for periodontal disease. It has been reported that reactive oxygen species linking both diseases, systemic melatonin supplementation as antioxidant therapy, was addressed as an adjuvant to scaling and root surface debridement (SRP) to enhance the treatment of periodontitis. Objective: To investigate the efficacy of systemic melatonin administration in periodontitis-obese patients as an adjuvant to scaling and root surface debridement (SRP). Methods: A randomized clinical trial was conducted at a dental-specialized center. Eighty subjects were included and allocated into group-I: twenty periodontium-healthy, normal-weight people; group-II: 30 obese patients with stage-III tre

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Publication Date
Wed Mar 04 2026
Journal Name
Alustath Journal For Human And Social Sciences
Musical relational in Andalusian poetry (Ibn al-Abar (d. 595 AH - 658 AH) as an example)
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The voice had a special place in the writting of the Andalusian poet (Ibn al-Abar ) , which aroused my attention because of the sonic capacity of the lettering inside the poetic at Ibn al-Abar poems . So Istudied the qualities of the lettering , structures and their exits . Scientists have not been able to determine the musical from the nonmusical sound , but we find the innate ability of Ibn al-Abar , which was able to determine this by using the lettering the right places and to revival the life to reflect the moments of his life , therefore came votes to express his purposes of praise and pride Etc. The poet Ibn al-Abar could exploit the lettering features in the effect of bilateral – static and moving and its ability to e

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Publication Date
Sun Oct 19 2025
Journal Name
Lecture Notes In Networks And Systems
Using Artificial Intelligence in Analyzing Historical Documents: The Egyptian Libyan Border as a Model (1911–1951)
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