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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
Fri Jun 23 2023
Journal Name
Cumhuriyet Dental Journal
The effectiveness of continuous versus sequential chelation in the removal of smear layer and their influence on push-out bond strength of Bio-C sealer (An in vitro study)
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Objectives: Successful endodontic treatment outcome requires effective shaping and cleaning of root canals. This study aims to evaluate the smear layer removal after continuous chelation (CC) ) NaOCL\HEDP( and sequential chelation (SC) )NaOCL\EDTA( and their influence on the push-out bond strength (POBS) of Bio-C sealer. Materials and Methods: Palatal roots of the maxillary first molar (n=72) were divided into four groups (n=18) as follows: 3% NaOCL, SC: 3% NaOCL followed by 17% EDTA, CC: 3% NaOCL \9% HEDP and Distilled water. Thirty-two roots (n=8/group) were split longitudinally for smear layer evaluation using SEM. Forty roots were obturated with Guttapercha and Bio-C sealer using a single cone technique. Thre

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Publication Date
Sat Sep 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the efficacy of ultrasound in the diagnosis of cervical lymphadenopathy
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Background: Cervical lymph nodes are prone to involved by a number of pathologic processes. They are common sites for lymphoma, metastasis, and reactive enlargement in a number of conditions. Aims of the study:-Clinical evaluation of patients with cervical lymphadenopathy. Differentiation between benign and malignant lymph nodes by means of ultra sounds (US) and Correlate the US findings with cytological and/or histopathological findings of cervical lymph nodes. Subjects, Materials and Methods:-The present study was carried out over a period of 6 months and included 81 patients of different age groups presenting with cervical lymphadenopathy. Each patient was examined clinically, then comprehensive sonographic examination of the neck for

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Publication Date
Sat Dec 31 2022
Journal Name
Al-kindy College Medical Journal
The Efficiency of Corn Solution as a Cytological Fixative in Buccal Smear : Corn Solution as Cytological Fixative
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Background: Corn Syrup is food syrup higher of carbohydrate, depending on grade. The study aimed to assess efficiency of Corn syrup as cytological fixative.

Subjects and methods: This was laboratory based study, it has been conducted at Elrazi University included   apparently 30 healthy students have been involved in this study.

Results: Out of 30 smears fixed with 95% alcohol, 76.7% (n=23) shows excellent nuclear stain, 23.3% (n= 7)   shows good nuclear stain. 70% (n=21) show excellent cytoplasmic stain, 26.7% (n=8) shows good cytoplasmic stain, 3.3% (n=1) shows poor cytoplasmuc stain.

   Out of 30 smears fixed with corn solution, 60

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
The Value of Ultrasonography in The Diagnosis and Evaluation of Early Therapeutic Response of Cervical Tuberculous Lymphadenitis
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ABSTRACT Background: Tuberculosis is a worldwide infectious disease in spite of advancement in health care system. Tuberculous lymphadenitis is the most prevalent form of extra pulmonary tuberculosis with predilection of cervical lymph nodes. Objectives: To evaluate the reliability of grey scale ultrasonography together with color Doppler in the diagnosis of cervical tuberculous lymph adenitis and evaluation of early therapeutic response. Subjects and methods:From July 2015 to May 2016 in Al-Karama teaching hospital /Kut city- Wasit-Iraq, 25 patients (14 males and 11 females) with ages range from (6-50) years. Ultrasonography examination was done for all patients and grey scale criteria (distribution, size, shape, echogenicity, echogenic hi

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Rationalization the costs of agricultural Activities under the use of genetic engineering: An applied research in ministry of agriculture - The directorate of inspection & certification of seeds
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The importance of this research has been to rationalize the cost of producing maize seeds through the followers of modern techniques and methods in agricultural activities such as genetic engineering for increasing production efficiency of maize seeds as well as the importance of calculating seed cost rationalization through the ABC system and thus rationalizing government spending. The research is based on one hypothesis in two ways that the use of genetic engineering on maize seeds works to: one - increase production efficiency of seeds and savings in agricultural inputs. 2. Rationalize the costs of examining and planting maize seeds. In order to calculate the costs will be based on the cost system based on activities ABC. The research

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Crossref
Publication Date
Fri Jul 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Performance Evaluation for Higher and Medium Leadership in Institutional Work Quality.
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Abstract:

This Research aims to define role of the system of evaluating the performance for higher leadership in determining the level of institutional work quality in the Ministry of Agriculture, by measuring system efficiency of evaluating the performance for higher leadership and its effect in institutional work quality, the searcher reached through the theoretical framing and involved studies to build default plan define the relation between Research variables formed from system of evaluating leadership performance as independent variable contains six subsidiary dimensions: (Polarization, evaluating the performance of personnel, training, motivation, se

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Publication Date
Wed Jun 01 2022
Journal Name
Resmilitaris
Evaluation mucin 1 polymorphism and expression with infertility in Iraqi females
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Scopus
Publication Date
Mon Jan 01 2024
Journal Name
Oral Health And Preventive Dentistry
Antioxidant and Antineoplastic Activities of Hibiscus sabdariffa Linn. Petal Extracts against Oral Squamous Cell Carcinoma Cell Line
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Purpose: To assess the antioxidant and antineoplastic effects of Hibiscus sabdariffa Linn. on oral squamous cell carcinoma cells. Materials and Methods: Human squamous cell carcinoma HSCC cells were tested for cytotoxicity by a methanol extract of Hibiscus sabdariffa (MEHSP). After 24, 48, and 72 ...

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Scopus (1)
Scopus
Publication Date
Tue Jan 03 2023
Journal Name
College Of Islamic Sciences
Narrative Structures in the Novel “Qiamat Baghdad” for the Novelist Alia Talib – Semiotic Study
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Abstract

The human mind knew the philosophy and logic in the ancient times, and the history afterwards, while the semiotics concept appeared in the modern time, and became a new knowledge field like the other knowledge fields. It deals, in its different concepts and references, with the processes that lead to and reveals the meaning through what is hidden in addition to what is disclosed. It is the result of human activity in its pragmatic and cognitive dimensions together. The semiotic token concept became a knowledge key to access all the study, research, and  investigation fields, due to its ability of description, explanation, and dismantling. The paper is divided into two sections preceded by a the

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Publication Date
Thu Oct 01 2020
Journal Name
Biochemical & Cellular Archives
RAPID SPECTROPHOTOMETRIC ESTIMATION OF TRACE AMOUNTS OF MEFENAMIC ACID BASED DISPERSIVE LIQUID-LIQUID MICROEXTRACTION OF IN PHARMACEUTICAL PREPARATIONS.
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A dispersive liquid-liquid microextraction combines with UV-V is spectrophotometry for the preconcentration and determination of Mefenamic acid in pharmaceutical preparation was developed and introduced. The proposed method is based on the formation of charge transfer complexation between mefenamic acid and chloranil as an n-electron donor and a p-acceptor, respectively to form a violet chromogen complex measured at 542 nm. The important parameters affecting the efficiency of DLLME were evaluated and optimized. Under the optimum conditions, the calibration graphs of standard and drug, were ranged 0.03-10 µg mL-1. The limits of detection, quantification and Sandell's sensitivity were calculated. Good recoveries of MAF Std. and drug at 0.05,

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