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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 Mar 03 2013
Journal Name
Baghdad Science Journal
Modifying Plaque assay and Clearance test as tools in determination of phage typing for E. Coli bacterial interspecies
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Bacteriophage of E. Coli interspecies from sewage samples were isolated , the phage particles were isolated from two different sewage samples . The first sample was collected from sewage sample of Baghdad university and the second sample was isolated from domestic sewage sample , first sample showed phages specialized for three E. Coli interspecies bacteria (first plate ) and two E. Coli interspecies bacteria (second plate ) , meanwhile second sample showed phage specialized for two E. Coli. interspeciesThe study of appearance of E coli phages from first sample showed three types of E. coli phages with different size of inhibition zone ( 1 , 0.7,0.5 )Cm respectively ( first plate ) , meanwhile E. Coli interspecies bacteria showed phages

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Publication Date
Fri Jul 01 2022
Journal Name
Journal Of Molecular Structure
Interaction behavior of curcumin encapsulated onto functionalized SBA-15 as an efficient carrier and release in drug delivery
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In this work, mesoporous silica SBA-15 was prepared and functionalized with amine groups (i.e., NH2) to form NH2/SBA-15. The curcumin (CUR) was encapsulated into the surface and pore of NH2/SBA-15 to create CUR@NH2/SBA-15 as an efficient carrier in drug delivery systems (DDSs). The three samples (i.e., SBA-15, NH2/SBA-15, and CUR@NH2/SBA-15) were characterized. The study investigated the effect of the carrier dose, initial CUR concentration, pH, and contact time on the CUR loading efficiency (DLE%) via adsorption. The best DLE% for the SBA-15 and NH2/SBA-15 were found to be 45% and 89.7%, respectively. The Langmuir isotherm had a greater correlation coefficient (R2) of 0.998 for SBA-15. A pseudo-secondorder kinetic model seemed to fit well

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Publication Date
Sun Oct 01 2017
Journal Name
Applied Energy
Hourly yield prediction of a double-slope solar still hybrid with rubber scrapers in low-latitude areas based on the particle swarm optimization technique
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Study of Plasma Metanephrine Level As Biochemical Parameter in Pregnant Women with Preeclampsia
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Pregnancy- including hypertension(PIH), also known as preeclampsia, is one of the major causes of maternal and fetal death. This study was carried out on 30 pregnant women with preeclampsia and 30 healthy pregnant women as control ranging in age mean ±SD (28.84±3.55) years , BMI (76.80±9.78) Kg/m2 and gestation age(30.82±0.75)week. The aim of this research was studied the plasma Metanephrine level and other biochemical parameters such as Hemoglobin(Hb), serum Protein, S. Albumin, Globulin, Albumin/Globulin ratio (Alb/Glu. ratio), S.Glutamate Pyruvate aminotransferase (GPT), S.Glutamate Oxaloacetate aminotransferase(GOT). The obtained results have been compared with 30 healthy pregnant women as control group. The result showed

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Publication Date
Sat Jun 01 2013
Journal Name
Journal Of The College Of Languages (jcl)
HONOUR " IN SOMERSET MAUGHAM 'S A MAN OF HONOUR MAUGHAM AS A DRAMATIST
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Somerset Maugham is known mainly as a novelist . This paper presents Maugham the dramatist . Many critics have found him a promising dramatist . He has written 30 plays , then he turns his back upon the theater and writes his autobiographical and most successful novel Of Human Bondage ( 1915) .

        Maugham's writing is clear , precise , and simple . He is described as a realist who is keenly aware of human nature , its concentration and frustration . His only tragedy A Man of Honour is a play in 4 acts . This paper concentrates mainly on this play to show Maugham as a dramatist and to show his concept of " honour " .

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Publication Date
Wed Feb 05 2014
Journal Name
Baghdad Science Journal
Study of Plasma Metanephrine Level As Biochemical Parameter in Pregnant Women with Preeclampsia
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Pregnancy- including hypertension(PIH), also known as preeclampsia, is one of the major causes of maternal and fetal death. This study was carried out on 30 pregnant women with preeclampsia and 30 healthy pregnant women as control ranging in age mean ±SD (28.84±3.55) years , BMI (76.80±9.78) Kg/m2 and gestation age(30.82±0.75)week. The aim of this research was studied the plasma Metanephrine level and other biochemical parameters such as Hemoglobin(Hb), serum Protein, S. Albumin, Globulin, Albumin/Globulin ratio (Alb/Glu. ratio), S.Glutamate Pyruvate aminotransferase (GPT), S.Glutamate Oxaloacetate aminotransferase(GOT). The obtained results have been compared with 30 healthy pregnant women as control group. The result showed that ther

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Publication Date
Sun Aug 01 2021
Journal Name
Journal Of Engineering
Reuse of Glass waste as a partial replacement to fine aggregates in concrete
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As human societies grow, the problem of waste management becomes one of the pressing issues that need to be addressed. Recycling and reuse of waste are effective waste management measures that prevent pollution and conserve natural resources. In this study, the possibility of using glass waste as an alternative was used as a partial weight substitute for fine aggregates with replacement ratios of 10, 20, 30, and 40% by the weight, and formed into test models (15 cm * 15 cm ) cube and (15 cm * 30 cm) cylinder, then matured and tested their strength compression and tensile strength at the age of 7 and 28 days and compared with a reference or conventional concrete with a mixing ratio (1: 1.5: 3) as well as testing its worka

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Publication Date
Mon May 28 2018
Journal Name
Iraqi Journal Of Science
Use Citrus aurantium plant as bio-indicator of air pollution in Baghdad city
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The current study was conducted to demonstrate the effects of air pollution on different biochemical parameters inCitrus aurantium plant and calculation the Air Pollution Tolerance Index (APTI). Five sites were selected tocollect plant leaves, four of them within the city of Baghdad, namely Al-Jadriya, Al-Andlous, Al-Doura and closeto the private generators to represent the urban areas and Abu Ghraib site to represent the rural area. Seasonalsamples were collected for the period from October 2016 to June 2017. Eleven biochemical parameters totalchlorophyll, ascorbic acid, leaf extract pH, relative water content, total nitrogen, total protein content, total sugarcontent, proline, electrical conductivity, cadmium and lead. The results of Citr

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Publication Date
Wed Sep 30 2020
Journal Name
College Of Islamic Sciences
The Breadth in the meaning of the "from Surah Maryam as a model.
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Prepositions have a key function, which is to associate parts of a sentence, called letters In addition, it adds the meanings of the verbs to the names, ie reached by them, and called by the coffin characters Qualities..

          I chose to search for the meaning of the preposition "from" in Surat Maryam to know its meanings in terms of originality and expansion, so the title of the research (the meanings of preposition "from" in terms of originality and expansion in Surat Maryam model(

 

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Publication Date
Tue Mar 15 2022
Journal Name
Al-academy
the indication of the scene as a symbolic system in the Iraqi theatrical
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The theatrical view reflects various connotations and intellectual and aesthetic implications, as the view includes a symbolic geometric, architectural and archetypal connotation suggestive of reality and nature, as theatrical art is the woman that reflects reality, specifically the significance of the theatrical view that reveals to us the philosophical, aesthetic and cognitive dimensions of theatrical trends, so the research came with the methodological framework, which It included the research problem (what is the significance of the scene as a symbolic system in the Iraqi theatrical performance), the importance of the research and the need for it, the research objective, the limits of the research and the most important terms.
A

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