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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
Tue Jan 01 2019
Journal Name
Current Research In Microbiology And Biotechnology
Detection of Anti-rubella virus, Cytomegalovirus and Chlamydia pneumonia antibodies in patients with type I diabetes mellitus
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Type-1 diabetes is defined as destruction of pancreatic beta cell, virus and bacteria are some environmental factor for this disease. The study included 25 patients with type-1 diabetes mellitus aged between 8 – 25 years from Baghdad hospital and 20 healthy persons as control group. Anti-rubella IgG and IgM, anti-Chlamydia pneumonia IgG and IgM were measured by ELISA technique while anti-CMV antibody were measured by immunofluorescence technique. The aim of current study was to know the trigger factor for type-1 diabetes. There were significant differences (P<0.05) between studied groups according to parameters and the results lead to suggest that Chlamydia pneumonia, CMV and rubella virus may trigger type-1 diabetes mellitus in Iraqi pat

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Biological Evaluation of Two New Analogues of Gonadotropin Releasing Hormone (GnRH)D-alanine8 and D-alanine
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So far synthesis of Gonadotropin Releasing Hormone (GnRH) analogues reported in the literature has clarified some aspects of structural activity of the naturally released GnRH. As a part of continuing efforts for further understanding of this relationship, the present investigation was undertaken which involved synthesis and biological evaluation of two GnRH analogues, firstly, by replacement of the amino acid L-Argenine in the 8th position at the backbone structure of the natural hormone by the amino acid D-Alanine; and secondly, by replacement of the amino acid L-Glycine in the 10th position by D-Alanine also at the backbone structure of the nature hormone, to obtain the following analogues respectively:

P

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Publication Date
Wed Jan 05 2022
Journal Name
Journal Of Nanomaterials
Green Synthesis of Silver Nanoparticles from Alhagi graecorum Leaf Extract and Evaluation of Their Cytotoxicity and Antifungal Activity
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Green synthesis of silver nanoparticles (AgNPs) using different plant parts has shown a great potential in medicinal and industrial applications. In this study, AgNPs were in vitro green synthesized using A. graecorum, and its antifungal and antitumoractivities were investigated. Scanning electron microscopy (SEM) image result indicated spherical shape of AgNPs with a size range of 22-36 nm indicated by using Image J program. The functional groups indicated by Fourier-transform infrared spectroscopy (FTIR) represented the groups involved in the reduction of silver ion into nanoparticles. Alhagi graecorum AgNPs inhibited MCF-7 breast cancer cell line growth in increased concentration depend manner, significant differences shown at

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Publication Date
Mon Jun 01 2020
Journal Name
Journal Of The College Of Languages (jcl)
Literature and Novel: Classical novel in comparison to New Novel By Alain Robbe - Grillet: L'Art et le Roman: Le Roman Traditionnel Face au Nouveau Roman Alain Robe- Grillet
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Modern French novel has gained a distinctive status in the history of French literature during the first half of the twentieth century. This is due to many factors including the new literary descriptive objective style adopted by novelists like Alain Robbe – Grillet that  has long been regarded as the outstanding writer of the nouveau roman, as well as its major spokesman, a representative writer and a leading theoretician of the new novel that has broken the classical rules of the one hero and evolved, through questioning the relationship of man and the world and  reevaluating the limits of contemporary fiction , into  creating a new form of narrative.

Résumé:

En vue de résu

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
In vitro MIC of Itraconazole Against Different Isolates of Candida albicans
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In vitro antifungal susceptibility test of itraconazole was carried out against 38 isolates from nails, skin, oral cavity, vagina and wounds, This study was done in Ramadi Teaching Hospital in period from January to August 2010. According to the National Committee for Clinical Laboratory Standard (NCCLS ) M 27- A by using the broth dilution method. Inoculum size was 1-5X103 CFU/ ml, while final concentrations of itraconazole ranged from 0.025 – 6.4 μg / ml by using RPMI – 1640 broth media and the fungus was incubated at 35 oC.  No resistant stain was recorded. MIC ranged from 0.05 – 6.4 μg / ml and the Mean ± SEM was 0.89 ± 0.28. MIC for nail isolates was 0.05 –

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Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Inhibitory Effects of Chalcone on the Replication of Poliovirus in Vitro
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The compound chalcon originally is extracted form some plant and herbs, the studies of the antiviral activity of this compound were done in two cell line cultures the L2OB and RD, the compound relatively non toxic to both cell lines of the concentration of 32?g/ml or less ,the compound have significantly anti poliovirus activity in both L2OB cell line and RD cell line, we find that the concentration of 0.03 ?g/ml or more inhibit the 100TCDID50 of the poliovirus .The therapeutic index(TI)used in this study to evaluate the drug activity ,( TI is the ratio of dose of drug which is just toxic to the cells to the does which is just inhibit the viral multiplication, if this index more than one the margin of safety of drug is according great ) .In

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Publication Date
Sat Feb 08 2014
Journal Name
Reaction Kinetics, Mechanisms And Catalysis
Kinetic and mathematical approaches to the corrosion of mild steel in nitric acid
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Publication Date
Tue Dec 29 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Separation and Identification of Phenolic Acid from Borago officinalis (F:Boraginaceae) Cultivated in Iraq
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    The plant Borago officinalis, which belongs to the Boraginaceae family and Celebrated as borage, is one of the useful medicinal plants cultivated in Iraq. It was used in olde medicine in Iraq, Irane, Syria and Europe for management of various diseases. It is commonly used as an atonic, tranquilliser, management of cough, sore throat, pneumonia, swelling, inflammatory diseases, antioxidant, and anticancer. This project provides the first comprehensive research done in Iraq to study the phytochemicals and the methods of extraction and isolation of active constituents from Borago officinalis cultivated in Iraq. The plant was harvested in spring from AL-Rifai, Nassiriyah city, IRAQ in February 2019.were w

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Publication Date
Mon Jun 30 2003
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Absorption of NO2 into Water and Nitric Acid Solutions in a Fixed Column
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Publication Date
Thu Mar 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Sensitivity of Streptococcus mutans to Selected Nanoparticles (in Vitro Study)
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Background: Nanoparticles are clusters of atoms in a size range from (1-100) nm. Nano dentistry creates amazing useful structures from individual atoms or molecules (nanoparticles), which provides a new alternative and a possibly superior strategy in prevention and treatment of dental caries through management of dental plaque biofilms. The aim of the study was to test the sensitivity of Streptococcus mutans to different concentrations of hydroxyapatite and iron oxide nanoparticles suspension solutions, in comparison to chlorhexidine, and de-ionized water, in vitro. Materials and methods: Agar well technique was applied to test the sensitivity of Streptococcus mutans to different concentrations of hydroxyapatite and iron oxide nanoparticle

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