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
Fri Feb 25 2022
Journal Name
Open Access Macedonian Journal Of Medical Sciences
Prospective Comparative Study of Fixing Displaced Transverse Patellar Fracture by Tension Band Wiring Versus Cannulated Screws with Wiring
...Show More Authors

BACKGROUND: Transverse fractures of the patella are important fractures with a wide variety of subtypes, the common incidence in the age group of 20–50 years. Surgical interference aims to achieve a perfect alignment of the joint surface, in addition to rigid fixation of the fracture for early re-habitation and early movement to retain the extensor mechanism of the knee joint. AIM: The aim of this study was to compare the radiological and functional outcomes of the displaced transverse patella fracture in adult patients treated by ORIF using tension band wiring versus cannulated screws with wiring. METHODS: A prospective analytic comparative study was conducted in Al-Kindy Teaching Hospital/Baghdad/Iraq for 18 months from Apr

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Fri Mar 15 2024
Journal Name
Journal Of Baghdad College Of Dentistry
A clinicopathological analysis of 151 odontogenic tumors based on new WHO classification 2022: A retrospective cross-sectional study
...Show More Authors

Background: Odontogenic tumors are a diverse group of lesions with a variety of clinical behavior and histopathologic subtypes, from hamartomatous and benign to malignant. The study aimed to examine the clinical and pathological features of odontogenic tumors in Baghdad over the last 11 years (2011–2021). Materials and Methods: The present retrospective study analyzed all formalin-fixed, paraffin-embedded tissue blocks of patients diagnosed with an odontogenic tumor that were retrieved from archives at a teaching hospital/College of Dentistry in Baghdad University, Iraq, between 2011 and 2021. The diagnosis of each case was confirmed by examining the hematoxylin and eosin stained sections by two expert pathologists. Data from pati

... Show More
Scopus (2)
Crossref (1)
Scopus Crossref
Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Terramechanics
Interaction of a rigid beam resting on a strong granular layer overlying weak granular soil: Multi-methodological investigations
...Show More Authors

In the geotechnical and terramechanical engineering applications, precise understandings are yet to be established on the off-road structures interacting with complex soil profiles. Several theoretical and experimental approaches have been used to measure the ultimate bearing capacity of the layered soil, but with a significant level of differences depending on the failure mechanisms assumed. Furthermore, local displacement fields in layered soils are not yet studied well. Here, the bearing capacity of a dense sand layer overlying loose sand beneath a rigid beam is studied under the plain-strain condition. The study employs using digital particle image velocimetry (DPIV) and finite element method (FEM) simulations. In the FEM, an experiment

... Show More
View Publication
Scopus (12)
Crossref (9)
Scopus Clarivate Crossref
Publication Date
Tue Oct 01 2019
Journal Name
Biochemical And Cellular Archives
α-TOCOPHEROL FOLIAR APPLICATION CAN ALLEVIATE THE ADVERSE EFFECT OF SALINITY STRESS ON WHEAT PLANT, TRITICUM AESTIVUM L.
...Show More Authors

Pots experiment was conducted at the greenhouse of botanical garden belong to Department of Biology, College of Education for Pure Science, Ibn-AL-Haithum, University of Baghdad, for growth season 2018-2019. The aim of the experiment was to study the effects of foliar application of a-tocopherol concentrations (0, 50, 100, 150, 200 mg.L-1) on growth parameters and the activity of some antioxidant enzymes of wheat plant irrigated with sodium chloride concentrations (0, 75, 150, 225) mM.L-1. Salinity reduced plant growth parameter, plant height, flag leaf area, flag leaf chlorophyll content and increased the activity of antioxidant enzymes, superoxide dismutase and peroxidase. Plant growth parameters were enhanced by foliar application of a-t

... Show More
Scopus (1)
Scopus
Publication Date
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Laser
Hong-Ou-Mandel Dip Measurements of Two Independent Weak Coherent Pulses for Free Space Quantum Key Distribution Systems
...Show More Authors

Preparation of identical independent photons is the core of many quantum applications such as entanglement swapping and entangling process. In this work, Hong-Ou-Mandel experiment was performed to evaluate the degree of indistinguishability between independent photons generated from two independent weak coherent sources working at 640 nm. The visibility was 46%, close to the theoretical limit of 50%. The implemented setup can be adopted in quantum key distribution experiments carried out with free space as the channel link, as all the devices and components used are operative in the visible range of the electromagnetic spectrum.

View Publication Preview PDF
Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
BIOCHEMICAL FEATURES of IRAQI PATIENTS INFECTED WITH HEPATITIS E VIRUS COMPARED WITH THOSE INFECTED WITH HEPATITIS A VIRUS
...Show More Authors

This study was designed to compare the effect of two types of viral hepatitis A and E (HAV
and HEV) on liver functions in Iraqi individuals by the measurement of biochemical changes
associated with hepatitis.
The study performed on 58 HEV and 66 HAV infected patients compared with 28 healthy
subjects. The measured biochemical tests include total serum bilirubin, serum transminases (ALT
and AST) alkaline phosphatase (ALP) and gamma glutamyl transferase (GGT).
The study showed that adolescent and young adults (17-29) years, were mostly affected by
HEV while children (5-12) years were frequently affected by HAV. The severity of liver damage in
HEV patients was higher than HAV patients as a result of high serum transa

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Feb 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
A Comparison of Parameters Estimation Methods for the Negative Binomial Regression Model under Multicollinearity Problem by Using Simulation
...Show More Authors

This study discussed a biased estimator of the Negative Binomial Regression model known as (Liu Estimator), This estimate was used to reduce variance and overcome the problem Multicollinearity between explanatory variables, Some estimates were used such as Ridge Regression and Maximum Likelihood Estimators, This research aims at the theoretical comparisons between the new estimator (Liu Estimator) and the estimators

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Mar 28 2021
Journal Name
Journal Of The College Of Education For Women
A Critical Discourse Analysis of Martin Crimp’s Piece “Advice to Iraqi Women”: عفراء عبد الحسين ناصر , سراب خليل
...Show More Authors

Language is a vehicle for social values and ideologies that a man intends or attempts to express. Dramatic texts are one of the discursive practices that embody values and ideologies. What is expressed in dramatic text is deliberate because it is meant to affect other’s values, trends and ideologies in one way or another. Such ideologies and values are not explicit. To bring them out requires putting language under scrutiny to unveil what is implied. The present study attempts to analyze a dramatic script entitled Advice to Iraqi Women by the British playwright Martin Crimp in an attempt to unveil the intended political ideologies underlying the text. The title reflects a political aspect embedded in the word “Iraqi” that

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Fri Dec 29 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Efficacy of Some Insect Growth Regulators (IGR) Against Jasmine White Fly Alearoclava Jasimini ( Homoptera: Aleyrodidae) on Citrus Tree
...Show More Authors

The efficacy of five insect growth regulators has been tested against white fly larva Alearoclava jasimini on citrus tree orchards. Data from field tl'ia ls con finned that percent mortalities were 43.7, 33.9, 23.7, 20.8 and     12.3  for  Admiral ( I miL)  pyriproxefen, Nomol t  1 5 SC  (!milL) Teflubenzuren , Match 050 EC (  I milL ) Lufenuren , cascade I 0 F.C (

0.9mi/L) flufenoxaron, and Dimiline 10 EC ( I milL)  Difluben- zuron. The result indicated that Admiral and Nomolt have a continuous  effect for one month , so the treatment needs to be repeated for each four weeks. Also, Admiral and Nomolt effect against eggs hatching by 41. 3 % and

    ... Show More
    View Publication Preview PDF
    Publication Date
    Thu Dec 24 2020
    Journal Name
    Advances In Civil Engineering
    Analytical study on torsional behavior of concrete beams strengthened with fiber reinforced polymer laminates using softened truss model
    ...Show More Authors

    This study aimed at evaluating the torsional capacity of reinforced concrete (RC) beams externally wrapped with fiber reinforced polymer (FRP) materials. An analytical model was described and used as a new computational procedure based on the softened truss model (STM) to predict the torsional behavior of RC beams strengthened with FRP. The proposed analytical model was validated with the existing experimental data for rectangular sections strengthened with FRP materials and considering torque-twist relationship and crack pattern at failure. The confined concrete behavior, in the case of FRP wrapping, was considered in the constitutive laws of concrete in the model. Then, an efficient algorithm was developed in MATLAB environment t

    ... Show More
    Scopus (6)
    Crossref (5)
    Scopus Clarivate Crossref