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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 13 2017
Journal Name
Al-khwarizmi Engineering Journal
Multi-Dimensional Angle of Arrival Estimation by Circular Phased Adaptive Array Antennas
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In this paper the use of a circular array antenna with adaptive system in conjunction with modified Linearly Constrained Minimum Variance Beam forming (LCMVB) algorithm is proposed to meet the requirement of Angle of Arrival (AOA) estimation in 2-D as well as the Signal to Noise Ratio (SNR) of estimated sources (Three Dimensional 3-D estimation), rather than interference cancelation as it is used for. The proposed system was simulated, tested and compared with the modified Multiple Signal Classification (MUSIC) technique for 2-D estimation. The results show the system has exhibited astonishing results for simultaneously estimating 3-D parameters with accuracy approximately equivalent to the MUSIC technique (for estimating elevation and a

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Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Antioxidant Activity of Endophytic Bacteria isolated from (Pyrrosia piloselloides) (L) M.G. Price
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Endophytic bacteria produced analogous secondary metabolites of their hosts. Similarly, the ability to generate antioxidants is not an exception. Dragon scales (Pyrrosia piloselloides), an epiphytic plant of the Polypodiaceae family, are frequently overlooked. This research aims to isolate antioxidant-producing bacteria from dragon-scale fern leaves. The antioxidant activities were tested after the extraction procedure using ethanolic extract. Bacteria were characterized and selected as candidates for antioxidant production by screening for the production of total phenolic compounds. Antioxidant levels were determined utilizing the ABTS, FRAP, and DPPH techniques. The preliminary findings of the entire phenolic compound test rev

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Publication Date
Wed Sep 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of Upper Removable Orthodontic Appliances on Oral Candidal Mucosal Carriage
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Background: Treatment of malocclusions using removable orthodontic appliances may prepare new stagnant areas susceptible for colonization and retention of Candida species, therefore; the aim of this study was to investigate the effect of upper removable orthodontic appliances on the mucosal Candidal count in group of apparently healthy orthodontic patients. Materials and Methods: Patients enrolled in this study were children aged 8-12 years having upper removable orthodontic appliances. Candidal counts at six mucosal sites were estimated using Imprint Culture method before, 14 and 28 days during orthodontic therapy. Results: Whole mouth and individual mucosal sites for Candidal counts increase significantly during treatment with upper remov

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Publication Date
Mon Dec 31 2018
Journal Name
Mustansiria Dental Journal
Management of Traumatized Permanent Maxillary Immature Incisor with Oblique Subgingival Crownroot Fracture
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Background: Trauma to the anterior teeth is a common injury in young children. Themaxillary incisors being the most affected. Although root fractures are rare, theydo occur and were previously and often considered hopeless and were extracted.The time between the injury and the initiation of treatment, level of the fractureline, and stage of root development are some criteria to be considered whenchoosing a treatment approach for a complicated tooth fracture. This case reportdescribes the management of a traumatized immature maxillary central incisorwith Elise class IV fracture with vertical oblique subgingival fracture of the root.Materials and method: Apexification was carried out using biodentine followed byremoval of the fracture

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Publication Date
Mon Nov 01 2021
Journal Name
Journal Of Ecological Engineering
Adsorption of Lead Ions from Aqueous Solutions onto Rice Husks, Continuous System
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Publication Date
Tue Dec 01 2020
Journal Name
Baghdad Science Journal
Numerical Solution of Fractional Volterra-Fredholm Integro-Differential Equation Using Lagrange Polynomials
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In this study, a new technique is considered for solving linear fractional Volterra-Fredholm integro-differential equations (LFVFIDE's) with fractional derivative qualified in the Caputo sense. The method is established in three types of Lagrange polynomials (LP’s), Original Lagrange polynomial (OLP), Barycentric Lagrange polynomial (BLP), and Modified Lagrange polynomial (MLP). General Algorithm is suggested and examples are included to get the best effectiveness, and implementation of these types. Also, as special case fractional differential equation is taken to evaluate the validity of the proposed method. Finally, a comparison between the proposed method and other methods are taken to present the effectiveness of the proposal meth

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Publication Date
Sun Mar 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Effect of Cold Atmospheric Pressure Plasma on Fertility Hormones for Female Rats
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Abstract<p>The direct application of cold atmospheric plasma (CAP) is the main scope of plasma medicine in or on the organism for curative purposes. Cold plasma is both effective in disrupting a wide range of microorganisms including multiple drug resistant ones (MDRs) and to stimulate proliferation of mammalian cells. It has obtained by Floating Electrode Dielectric Barrier Discharge (FE-DBD) system. The present study aimed to show the effected of cold plasma on the fertility hormones LH, Prolactin, Estrogen, and Testosterone hormones for healthy adult female rats (Albino) / bulb c). There are divided into many groups according to time exposure of plasma (15, 30, 60, and 90 second) and a refere</p> ... Show More
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Publication Date
Wed Jan 01 2020
Journal Name
Indian Journal Of Forensic Medicine And Toxicology
Color stability of different aesthetic resin composite materials: A digital image analysis
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Publication Date
Mon Nov 01 2010
Journal Name
Journal Of Systems And Software
Development of Java based RFID application programmable interface for heterogeneous RFID system
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Publication Date
Fri Dec 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Phylogenetic Relationship of Iraqi Vespa orientalis Linnaeus 1771 Wasps Using Mitochondrial CO1
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Abstract<p>Oriental wasps are scavengers, and they have also represented an enormous issue for beekeepers, they destroy beehives and reduce the flight of bees. In addition, the sting of hornets may cause medical problems, which differ according to the response of the individuals, including severe sensitivity, swelling, and slight pain. This study provides the first molecular phylogeny of the oriental wasp <italic>Vespa orientalis</italic> L. in Iraq. Mitochondrial DNAs of the 547bp fragment cytochrome oxidase subunit 1 (CO1) area were sequenced and analyzed from 10 wasp specimens collected in the north, middle, and south of Iraq. The CO1 gene found in the Iraqi isolates was used to cre</p> ... Show More
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