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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 Jun 01 2011
Journal Name
Journal Of The College Of Languages (jcl)
Новые направления и течения начала Серебряного века The Silver Age and the New Trends That appeared at the Twentieth Century.
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    Годы, принадлежащие концу XIX – началу XX столетия, вошли в русскую литературу под красивым названием Серебряный век. В это время в стране появился целый ряд выдающихся поэтов, имена которых навсегда останутся в русской и мировой литературе. Это Ахматова, Гумилев, Блок, Маяковский и многие другие. Все эти люди творили в нелегкое для России время. Началом Серебряного века условно считают 189

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Publication Date
Wed Mar 07 2018
Journal Name
Journal Of Cellular And Molecular Medicine
Resveratrol protects mice against SEB‐induced acute lung injury and mortality by miR‐193a modulation that targets TGF‐β signalling
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Abstract<p>Staphylococcal enterotoxin B (SEB) is a potent superantigen produced by <italic>Staphylococcus aureus</italic> that triggers a strong immune response, characterized by cytokine storm, multi‐organ failure, and often death. When inhaled, SEB can cause acute lung injury (ALI) and respiratory failure. In this study, we investigated the effect of resveratrol (RES), a phytoallexin, on SEB‐driven ALI and mortality in mice. We used a dual‐exposure model of SEB in C3H/HeJ mice, which caused 100% mortality within the first 5 days of exposure, and treatment with RES resulted in 100% survival of these mice up to 10 days post‐SEB exposure. RES reduced the inflammatory cytokines in the serum an</p> ... Show More
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Publication Date
Fri May 31 2019
Journal Name
Journal Of Engineering
Water Retention Techniques under Crop’s Root Zone a Tool to Enhance Water Use Efficiency and Economic Water Productivity for Zucchini
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 A new technique in cultivation by installing membrane sheet below the crop’s root zone was helped to save irrigation water in the root zone, less farm losses, increasing the field water use efficiency and water productivity. In this paper, the membrane sheet was installed below the root zone of zucchini during the summer growing season 2017 in open field.  This research was carried out in a private field in Babil governorate at Sadat Al Hindiya Township reached 72 km from Baghdad. Surface trickle irrigation system was used for irrigation process. Two treatment plots were used, treatment plot T1 using membrane sheet and treatment plot T2 without using the membrane sheet. The applied irrigation water, time of

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Publication Date
Mon Jun 01 2015
Journal Name
. International Journal Of Computer Science And Mobile Computing
A Hybrid Lossy Image Compression based on Wavelet Transform, Polynomial Approximation Model, Bit Plane Slicing and Absolute Moment Block Truncation
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Publication Date
Thu Jan 31 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Analysis the Expected Profit By the Relation Between the Sustainable growth and Actual growth: Apply Study for Iraq Stock Exchange
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The research aims to analysis the future profits of companies listed on the Iraq Stock Exchange through analyzing the relationship between Actual Growth and Sustainable Growth, The study was applied to the sample of companies included in the Iraq Stock Exchange for the period (2010- 2014), The Internal Growth Rate has been used as a measure for the Actual Return Rate but the Sustainable Growth Rate has been measured under the Rose model, The research showed group of conclusions, the most important are:1. From the analysis of sustainable growth for the banks sample and the variables involved in its measure shows that investment in the investors amounts have achieved a significant return, which demonstrates the company's efficiency at gene

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Publication Date
Fri Feb 10 2023
Journal Name
Energies
Well Placement Optimization through the Triple-Completion Gas and Downhole Water Sink-Assisted Gravity Drainage (TC-GDWS-AGD) EOR Process
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Gas and downhole water sink-assisted gravity drainage (GDWS-AGD) is a new process of enhanced oil recovery (EOR) in oil reservoirs underlain by large bottom aquifers. The process is capital intensive as it requires the construction of dual-completed wells for oil production and water drainage and additional multiple vertical gas-injection wells. The costs could be substantially reduced by eliminating the gas-injection wells and using triple-completed multi-functional wells. These wells are dubbed triple-completion-GDWS-AGD (TC-GDWS-AGD). In this work, we design and optimize the TC-GDWS-AGD oil recovery process in a fictitious oil reservoir (Punq-S3) that emulates a real North Sea oil field. The design aims at maximum oil recovery us

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Publication Date
Tue May 16 2023
Journal Name
Journal Of Engineering
Experimental Study For a Laminar Natural Convection Heat Transfer From an Isothermal Heated Square Plate With and Without Circular Hole
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An experimental investigation of natural convection heat transfer from an isothermal horizontal,vertical and inclined heated square flat plates with and without circular hole, were carried out in two cases, perforated plates without an impermeable adiabatic hole "open core" and perforated plates with an impermeable adiabatic hole "closed core" by adiabatic plug. The experiments covered the laminar region with a range of Rayleih number of (1.11x106 ≤RaLo≤4.39x106 ), at Prandtle number (Pr=0.7). Practical experiments have been done with variable inclination angles from horizon (Ф=0o ,45o,90o,135oand 180o),facing upward (0o≤Ф<90o), and downward (90o
≤Ф<180o). The results showed that the temperature gradient increases whi

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Publication Date
Fri Jan 01 2016
Journal Name
Journal Of The College Of Languages (jcl)
Investigating English Composition Writing Problems Encountered by Preparatory School Students and Finding Solutions to These Problems through Schema- Based Approach
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Writing in English is one of the essential factors for successful                      EFL learning .Iraqi students at the preparatory schools encounter problems when using their background knowledge in handling subskills                                  of writing(Burhan,2013:164).Therefore, this study aims to investigate the 4thyear preparatory school students’ problems in English composition writing, and find solutions to these pro

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Publication Date
Mon Nov 20 2028
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
DETERMINATION OF OPTIMAL CONDITIONS FOR CAROTENOIDS PRODUCTION BY CHEMICAL MUTANAT LOCAL ISOLATE RHODOTORUL MUCILAGENOSA M.: DETERMINATION OF OPTIMAL CONDITIONS FOR CAROTENOIDS PRODUCTION BY CHEMICAL MUTANAT LOCAL ISOLATE RHODOTORUL MUCILAGENOSA M.
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The aim of this study was to increasing natural carotenoides production by a locally isolate Rodotorula mucilagenosa M. by determination of the optimal conditions for growth and production of this agents, for encouragest to use it in food application permute artificial pigments which harmfull for consumer health and envieronmental. The optimal condition of carotenoides production from Rhodotorula mucilaginosa M were studied. The results shows the best carbon and nitrogen source were glucose and yeast extract. The carotenoids a mount production was 47430 microgram ̸ litter and 47460 microgram ̸ litter, respectively, and the optimum temperature was 30°C, PH 6, that the carotenoides a mount was 47470 microgram ̸ litter and 47670 microgr

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Publication Date
Thu Jan 16 2025
Journal Name
Journal Of Biological Control
Toxicity of polymeric nanocapsules prepared from &lt;i&gt;Moringa oleifera&lt;/i&gt; leaf extract against the larvae of &lt;i&gt;Culex pipiens&lt;/i&gt; (Diptera: Culicidae)
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The study aimed to prepare a nanocapsules formulation from the acetonic extract of Moringa oleifera leaves, using polymeric capsules, and test its toxicity against the third instar larvae of Culex pipiens mosquitoes. The leaf extract was prepared using acetone as a solvent, and the nano polymeric capsules were prepared using the synthetic polymer polyethylene glycol 4000. The results showed the successful preparation of nano polymeric capsules from the leaf extract, with an average particle size of 259.2 nm, and a nanocapsule diameter of 263.83 nm, as determined by DLS and SEM analysis, respectively. The toxicity results indicated that the nano polymeric capsules of the leaf extract exhibited higher mortality rates, reaching 97.6% a

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