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
Wed Aug 31 2022
Journal Name
International Journal Of Intelligent Engineering And Systems
Performance Evaluation Based on Multi-UAV in Airborne Computer Network System
...Show More Authors

View Publication
Scopus (4)
Crossref (1)
Scopus Crossref
Publication Date
Mon Dec 30 2024
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Formation evaluation for Mauddud Formation in Bai Hassan oilfield, Northern Iraq
...Show More Authors

   Formation evaluation is a critical process in the petroleum industry that involves assessing the petrophysical properties and hydrocarbon potential of subsurface rock formations. This study focuses on evaluating the Mauddad Formation in the Bai Hassan oil field by analyzing data obtained from well logs and core samples. Four wells were specifically chosen for this study (BH-102, BH-16, BH-86, and BH-93). The main objectives of this study were to identify the lithology of the Mauddud Formation and estimate key petrophysical properties such as shale volume, porosity, water saturation, and permeability. The Mauddud Formation primarily consists of limestone and dolomite, with some anhydrites present. It is classified as a clean for

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jun 01 2020
Journal Name
Journal Of The College Of Languages (jcl)
OUTDATED VOCABULARY in A. I. HERZEN's NOVEL " who is to BLAME?": УСТАРЕВШАЯ ЛЕКСИКА В РОМАНЕ А. И. ГЕРЦЕНА «КТО ВИНОВАТ?»
...Show More Authors

The article considers the main reason for A. I. Herzen's address to obsolete words, which is their ability to acquire a stylistic coloring in the context of speech, as well as the possibility of combining, in some cases, with neutral lexemes of various functional styles. A certain stylistic effect of such characteristics of this type of vocabulary is represented, as a result of which their stylistic coloring in syntagmatic terms does not coincide with stylistic coloring in terms of paradigmatics, that is, in speech they have a completely stylistic meaning. Attention is focused on the role of outdated vocabulary, which consists in the fact that they serve to implement such features of the artistic style as imagery, emotionality, and their

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Mar 18 2021
Journal Name
Review Of International Geographical Education Online
Chomsky's Political Views as a Case Study in a Critical Discourse Analysis of Ideology in the Iraqi Wars
...Show More Authors

APDBN Rashid, Review of International Geographical Education Online (RIGEO), 2021

View Publication
Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

Scopus (10)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

View Publication
Scopus (10)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synergistic Effects of 2-Deoxy-D-Glucose and Cinnamic Acid with Erlotinib on NSCLC Cell Line
...Show More Authors

Background: In spite of all efforts, Non-small cell lung cancer (NSCLC) is a fatal solid tumor with a poor prognosis as of its high metastasis and resistance to present treatments. Tyrosine kinase inhibitors (TKI) such as erlotinib are efficient in treating NSCLC but the emergence of chemoresistance and adverse effects substantially limits their single use. Objective: in this study, the combination treatments of either 2-deoxy-D-glucose (2DG) or cinnamic acid (CINN) with erlotinib (ERL) were tested for their possible synergistic effect on the proliferation and migration capacity of NSCLC cells. Methods: In this study, NSCLC model cell line A549 was used to investigate the effects of single compounds and their combination on cell gro

... Show More
View Publication
Scopus (5)
Crossref (3)
Scopus Crossref
Publication Date
Sun Jan 01 2023
Journal Name
Chemical Methodologies
Cytotoxicity and Anticancer Effect of Chitosan-Ag NPs-Doxorubicin-Folic Acid Conjugate on Lungs Cell Line
...Show More Authors

This study looked at how the synthetic chitosan-AgNPs-Doxorubicin-folic acid combination affected the A549 cell line in terms of cytotoxicity and anticancer activity. By reducing silver nitrate (AgNO3) and biodegradable chitosan, silver nanoparticles were biosynthesized. The produced conjugate was examined by using FT-IR spectroscopy, atomic force microscopy (AFM), and field emission scanning electron microscopy (FE-SEM). The cytotoxicity assay for the viability of A549 cells revealed that the combination of chitosan, AgNPs, doxorubicin, and folic acid decrease cell viability in a dose-determined by method over 48 hours, which direct to a dependent reduce in the activity of A549 cells. The mechanism analysis of the impacted living cells lea

... Show More
View Publication Preview PDF
Scopus (30)
Scopus
Publication Date
Mon Mar 13 2023
Journal Name
Diagnostics
The Effect of a Bioactive Oral System and CO2 Laser on Enamel Susceptibility to Acid Challenge
...Show More Authors

This study evaluated the structural changes of enamel treated by the Regenerate system and carbon dioxide (CO2) laser against acid challenge. Thirty human enamel slabs were prepared and assigned into three groups: Group I: untreated (control); Group II: treated with the Regenerate system; and Group III exposed to CO2 laser. All specimens were subjected to an acid challenge (pH 4.5–7.0) for 14 days. Specimens were evaluated and compared at 120 points using five Raman microspectroscopic peaks; the phosphate vibrations ν1, ν2, ν3, and ν4 at 960, 433, 1029, and 579 cm−1, respectively, and the carbonate at 1070 cm−1, followed by Vickers microhardness test. The ratio of carbonate to phosphate was correlated to the equivalent mic

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (6)
Scopus Clarivate Crossref
Publication Date
Wed Feb 14 2024
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

View Publication
Scopus (10)
Crossref (10)
Scopus Crossref