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
Thu Oct 01 2020
Journal Name
Test Engineering & Management
Strengthening of non-liner finite element RCMD Beam with Large Square Opening Using CFRP
...Show More Authors

Publication Date
Wed Dec 01 2021
Journal Name
Iraqi Journal Of Physics
Optical, Structural, Morphological Properties of Chromium (III) Oxide Nanostructure Synthesized Using Spray Pyrolysis Technique
...Show More Authors

Nanostructure of chromium oxide (Cr2O3-NPs) with rhombohedral structure were successfully prepared by spray pyrolysis technique using Aqueous solution of Chromium (III) chloride CrCl3 as solution. The films were deposited on glass substrates heated to 450°C using X-ray diffraction (XRD) shows the nature of polycrystalline samples. The calculated lattice constant value for the grown Cr2O3 nanostructures is a = b = 4.959 Å & c = 13.594 Å and the average crystallize size (46.3-55.6) nm calculated from diffraction peaks, Spectral analysis revealed FTIR peak characteristic vibrations of Cr-O Extended and Two sharp peaks present at 630 and 578 cm-1 attributed to Cr-O “stretching

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Thu Jan 13 2022
Journal Name
Medical & Biological Engineering & Computing
An integrated entropy-spatial framework for automatic gender recognition enhancement of emotion-based EEGs
...Show More Authors

View Publication
Scopus (15)
Crossref (14)
Scopus Clarivate Crossref
Publication Date
Wed Feb 03 2021
Journal Name
Structural Concrete
Finite element analysis of rectangular RC beams strengthened with FRP laminates under pure torsion
...Show More Authors

Scopus (24)
Crossref (18)
Scopus Clarivate Crossref
Publication Date
Thu Sep 30 2004
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Simulation the Radiation Zone of Al-Mussaib Power Plant by using Monte Carlo Method
...Show More Authors

View Publication Preview PDF
Publication Date
Wed Jun 30 2021
Journal Name
International Journal Of Intelligent Engineering And Systems
Promising Gains of 5G Networks with Enhancing Energy Efficiency Using Improved Linear Precoding Schemes
...Show More Authors

Scopus (2)
Scopus Crossref
Publication Date
Fri Dec 01 2023
Journal Name
Political Sciences Journal
Exploring the Effects of European Union Conditionality Language on European Mediterranean Human Rights Dialogue
...Show More Authors

Since more than a decade, human rights dialogue in the European Mediterranean Region has been marked by a number of tensions. Although a number of factors contribute to such disputes, the effect of human rights conditionality, which ties EU economic cooperation progression with partner countries human rights advancement, on the dialogue has not been studied. Understanding the aspects, impacts, and effects of conditionality on Euro-Med relations is crucial for furthering dialogue. Yet this variable has been almost entirely neglected in academic and policy research. The research concludes several direct and indirect impacts of conditionality on human rights dialogue using a mixed methodology approach. Direct effects are reflected in the wi

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Sep 28 2023
Journal Name
Iraqi Journal Of Computer, Communication, Control And System Engineering
Distinct Architectures of Feed Forward Neural Network for Implementing A Human Swing Leg System
...Show More Authors

The artificial intelligence techniques such as neural networks and fuzzy systems play an important role to disconnect flexion & expansion of the swing leg, the earth response force of the other foot has been redesigned. Under that paper, we think the fuzzy controller plan issue for yield following flawed genuine investigation of nonlinear systems. For examination, an essential fuzzy control plot has been bristly developed dependent on a current methodology delegate under the field. In this paper, the Feedforward Neural Network has been implemented with integer, fixed point and floating point data representations. Additionally, The Fuzzy Logic Controllers in both analog and digital forms has been implemented in hardware. Both designs use les

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Thu Dec 01 2011
Journal Name
Iraqi Journal Of Physics
Design of Achromatic Combined Quadrupole Lens Using the Modified Bell-Shaped Field Distribution Model
...Show More Authors

The optimization calculations are made to find the optimum properties of combined quadrupole lens consist of electrostatic and magnetic lenses to produce achromatic lens. The modified bell-shaped model is used and the calculation is made by solving the equation of motion and finding the transfer matrices in convergence and divergence planes, these matrices are used to find the properties of lens as the magnification and aberrations coefficients. To find the optimum values of chromatic and spherical aberrations coefficients, the effect of both the excitation parameter of the lens (n) and the effective length of the lens into account as effective parameters in the optimization processing

View Publication Preview PDF
Publication Date
Wed Dec 29 2021
Journal Name
Al-khwarizmi Engineering Journal
Analysis of Magnetorheological Normally Close Directional Control Valve: Magnetorheological normally close directional control valve
...Show More Authors

This valve is intended for use in valves for steering movement, using the qualities of the Magneto-rheological (MR) fluid to regulate the fluid, direct contact without the utilization of moving parts like a spool, a connection between electric flux, and fluid power was made, The simulation was done to employ the" finite element method of magnetism (FEMM)" to arrive at the best design. This software is used for magnetic resonance valve finite element analysis. The valve's best performance was obtained by using a closed directional control valve in the normal state normally closed (NC) MR valve, with simulation results revealing the optimum magnetic flux density in the absence of a current and the shedding condition, as well as the optimum

... Show More
View Publication Preview PDF
Scopus (2)
Scopus Crossref