Preferred Language
Articles
/
mRd8LZIBVTCNdQwC3KcL
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
...Show More Authors
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.

Scopus Clarivate Crossref
View Publication
Publication Date
Sun Jun 03 2012
Journal Name
Baghdad Science Journal
Study the effect of the mixture aquatic extract of Peganum harmala seeds and Pericarp of Punica granutum on viability of protoscolices of Echinococcus granulosus in vitro and in vivo
...Show More Authors

This study included the preparation of the mixture aquatic extracts of Peganum harmala seeds and Pericarp of Punica granutum at concentration (10+50) ?(15+55)? (20+60) mgml .To study the influence of the mixture on the percentage of vitality of the protoscolices of E. granulosus In vitro, as the vitality of protoscolices had caused complete death when the using concentration at time 120,90,60 minute respectively. Also study the effect of mixture in white mice with infectious protoscolices In vivo and study the change occurred in the averages of the weights of the liver and spleen and the averages of its distension In vivo in processed group with mixture at concentration (15+55) , (10+50)mgml ,as which was approach to the negative gro

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
The role of some types of erythrocytes on the growth of Entamoeba histolytica trophozoite in vitro
...Show More Authors

The parasite E.histolytica was first isolated from a stool sample, and then cultivated and maintained in vitro using Locke-egg medium (LEM) and Liver infusion agar medium (LIAM) . Then, the effect of some types of erythrocytes (human and sheep), on the growth and activity of the parasite in the two culture media was investigated. The parasite was able to ingest and lysis erythrocytes of human and sheep that were supplemented to the culture media and such manipulation was able to augment the reproduction rate of the cultivated E. histolytica, however, such consequence was media- and concentration-dependent. The reproduction rate was significantly increased (66.0, 57.5 and 58.6%, respectively) in LEM medium containing human erythrocytes ty

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Dec 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of Enamel Surface after Debonding of Different Types of Esthetic Brackets (An In Vitro Study)
...Show More Authors

Background: Debonding orthodontic brackets and removal of residual bonding material from the enamel surface include critical steps that may cause enamel damage. The aim of the present study was to evaluate and compare the site of bond failure and enamel surface damage after debonding of three types of esthetic brackets (composite, ceramic, sapphire) bonded with light cure composite and resin-modified glass ionomer adhesive. Materials and methods: Seventy two maxillary premolars teeth were divided into three groups each group consisted of 24 teeth according to the type of brackets. Each group was subdivided into two subgroups (12 teeth for each) according to the bonding material that was used. After 7 days of bonding procedure, the brackets

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Apr 30 2023
Journal Name
Iraqi Journal Of Science
Detection of A Possible Subsurface Water Seepage Using 2D Electrical Resistivity Imaging Survey at a site in Al-Khwarizmi College of Engineering, University of Baghdad, Iraq
...Show More Authors

     Unknown subsurface leaking water sources and possible subsurface seepage from a sewage tank in a garden at Al-Khawarizmi engineering college, University of Baghdad, were detected in this study. The 2D electrical resistivity imaging. The ERI survey is carried out along two lines, 60m and 50m long, with an electrode spacing of 1 m, forming a cross using the Wenner-Schlumberger array configuration. Line 1 is 60m, while line 2 is 50m. Soil samples were collected from line 1 at positions of electrode 34, which shows a high resistivity value, and electrode 55, which shows low resistivity, for laboratory analysis. Robust inversion and modelling processes showed relative change and high contrast in interpreted resistivities. Soil analy

... Show More
View Publication Preview PDF
Scopus (1)
Scopus Crossref
Publication Date
Wed Feb 05 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Expression of Ki67 and p53 as proliferation and apoptosis markers in adenoid cystic carcinoma
...Show More Authors

Background: Adenoid cystic carcinoma (ACC) constitutes about 4% of salivary epithelial tumors and is the second common malignant epithelial salivary gland tumor involving both the major and minor salivary glands. Aims of the study is to evaluate immunohistochemical expression of Ki67 and p53 proteins in ACC. Materials and Methods: immunohistochemical analyses of fifteen cases of formalin – fixed paraffin – embedded tissues blocks of ACC of salivary glands using ki67 and p53 antibodies. Results: ki67 was expressed in 6 of 15 ACC (40%) while p53 aberration was demonstrated in 11 of tumor (73.3%). There was a statistically significant difference between the expression of ki67 and p53 proteins in ACC cases (p value = 0.041). Pearson’s cor

... Show More
View Publication Preview PDF
Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis of Bimetallic Au–Pt / TiO2 Catalysts as an Efficient Catalyst for the Photodegradation of Crystal Violet Dye
...Show More Authors

     Bimetallic Au –Pt catalysts supporting TiO2 were synthesised using two methods; sol immobilization and impregnation methods. The prepared catalyst underwent a thermal treatment process at 400 C, while the reduction reaction under the same condition was done and the obtained catalysts were identified with transmission electron microscopy (TEM) and energy-dispersive spectroscopy (EDS). It has been found that the prepared catalysts have a dimension around 2.5 nm and the particles have uniform orders leading to high dispersion of platinum molecules .The prepared catalysts have been examined as efficient photocatalysts to degrade the Crystal violet dye under UV-light. The optimum values of Bimetallic Au –

... Show More
View Publication Preview PDF
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Sun Mar 15 2020
Journal Name
Journal Of The College Of Education For Women
The Use of English as Lingua Franca in the Classes of UKM: as A Case of Study
...Show More Authors

           English has for long been one of the most widely used media of communication globally, especially in the Malaysian universities. It has been termed as a Lingua Franca because it is shared with other languages which are considered first languages by different speakers. For this reason, English as a Lingua Franca (ELF) has attracted a number of researchers to investigate its variety via other languages in various communities. The objective of this paper is therefore to establish the strategies which are employing by the international students at the National University of Malaysia/ UniversitiKebangsaan Malaysia (UKM) as an example of one of the Malaysian universities; when they e

... Show More
View Publication Preview PDF
Publication Date
Wed Aug 30 2023
Journal Name
Iraqi Journal Of Science
In vitro Radio Protective Effects of Metformin on Human Lymphocytes Irradiated with Gamma Rays
...Show More Authors

     Radio protective effects of metformin and its ability to alter the spontaneous and induced genotoxic and cytotoxic levels effects on human peripheral blood lymphocytes were investigated in this study. Metformin, a hypoglycemic oral drug,  is a biguanide derived from Galega officinalis that is widely utilized in controlling type 2 diabetes mellitus. Whole blood samples from 10 healthy donors (5 males and 5 females) were exposed to two doses of gamma-rays (1 and 2 Gray). Lymphocytes in cultures were treated with metformin (10 and 50µM) before gamma-irradiation. Cytokinesis-block micronucleus test was used to evaluate the protective effects of metformin on radiation induced genomic damage, cytostasis and

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Sun Apr 30 2023
Journal Name
Iraqi Journal Of Science
Screening for in Vitro Biofilm Formation Ability of Locally Isolated Uropathogenic Escherichia coli (UPEC)
...Show More Authors


Seventy-six urine specimens were collected from of patients suffering from recurrent
urinary tract infections (UTIs). Specimens were bacteriologically analyzed, fifty
(65.8%) of isolated bacterial strains were belonged to E.coli. 100% of isolated
uropathogenic E.coli (UPEC)strains displayed a biofilm positive phenotype under
optimized condition using microtiter plate assay. 21 of E.coli strains classified as highly
positive biofilm producers (42%), and 29 (58%) as weakly positive biofilm producers.

View Publication Preview PDF
Publication Date
Wed Dec 01 2021
Journal Name
Iraqi Journal Of Science
Effect of silver nanoparticles on macrophage cytotoxicity upon exposure to Leishmania tropica in vitro
...Show More Authors

Cutaneous leishmaniasis (CL) is the most form of leishmaniasis disease prevalent in Iraq. CL remains a public health problem in numerous endemic countries because of the absence of safe, effective, and high-cost drugs for treatment. Macrophages are the main inhabitant cell for Leishmania; they phagocyte and allow parasite multiplying. Phagocytosis and anti-leishmanial activity of macrophage are the main factors in the elimination of Leishmania parasites. Phagosome-resident amastigotes also evade innate host defense mechanisms. Silver nanoparticles (Ag NPs) have an important effect in stimulating the production of oxygen species. The objective of this study was to examine macrophages cytotoxicity upon exposure to L. tropica and Ag NPs. Se

... Show More
View Publication Preview PDF