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 Dec 20 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Sulfur Derivatives of 1,2,4-Triazole: Recently Developed Compounds, Structure Activity Relationship, and Biological Activity: Review article
...Show More Authors

The term of heterocyclic chemistry focuses only on heterocyclic compounds, which consider as a percentage of organic chemistry, they equal to greater than sixty-five. These compounds are widely founded in nature and most of them are important to life. In the past few years, scientist fused on 1,2,4-triazoles and their condensed heterocyclic ring due to their medicinal significance, 1,2,4-triazole containing Sulphur atom is one of the important heterocyclic moieties due to its broad range of biological activities also their derivatives can accommodate one of the alternatives as electronic effect as exchanges of the electronic density (electron donating or withdrawing) groups ; for all what mentioned above they are consider as a core

... Show More
View Publication
Scopus (2)
Crossref (1)
Scopus Crossref
Publication Date
Sun Jun 01 2014
Journal Name
International Journal Of Advanced Research In Computer Science And Software Engineering
Medical Image Compression using Wavelet Quadrants of Polynomial Prediction Coding & Bit Plane Slicing
...Show More Authors

Publication Date
Sat Jan 01 2022
Journal Name
Proceedings Of International Conference On Computing And Communication Networks
Automatic Health Speech Prediction System Using Support Vector Machine
...Show More Authors

View Publication
Scopus (3)
Scopus Clarivate Crossref
Publication Date
Fri May 01 2020
Journal Name
Journal Of Electrical And Electronics Engineering
HF Wave Propagation Prediction Based On Passive Oblique Ionosonde
...Show More Authors

High frequency (HF) communications have an important role in long distances wireless communications. This frequency band is more important than VHF and UHF, as HF frequencies can cut longer distance with a single hopping. It has a low operation cost because it offers over-the-horizon communications without repeaters, therefore it can be used as a backup for satellite communications in emergency conditions. One of the main problems in HF communications is the prediction of the propagation direction and the frequency of optimum transmission (FOT) that must be used at a certain time. This paper introduces a new technique based on Oblique Ionosonde Station (OIS) to overcome this problem with a low cost and an easier way. This technique uses the

... Show More
View Publication Preview PDF
Scopus
Publication Date
Mon Sep 30 2024
Journal Name
Iraqi Journal Of Science
Attention-Deficit Hyperactivity Disorder Prediction by Artificial Intelligence Techniques
...Show More Authors

Attention-Deficit Hyperactivity Disorder (ADHD), a neurodevelopmental disorder affecting millions of people globally, is defined by symptoms of hyperactivity, impulsivity, and inattention that can significantly affect an individual's daily life. The diagnostic process for ADHD is complex, requiring a combination of clinical assessments and subjective evaluations. However, recent advances in artificial intelligence (AI) techniques have shown promise in predicting ADHD and providing an early diagnosis. In this study, we will explore the application of two AI techniques, K-Nearest Neighbors (KNN) and Adaptive Boosting (AdaBoost), in predicting ADHD using the Python programming language. The classification accuracies obtained w

... Show More
View Publication Preview PDF
Scopus (8)
Crossref (4)
Scopus Crossref
Publication Date
Wed Feb 01 2023
Journal Name
Journal Of Engineering
Vertical Stress Prediction for Zubair Oil Field/ Case Study
...Show More Authors

Predicting vertical stress was indeed useful for controlling geomechanical issues since it allowed for the computation of pore pressure for the formation and the classification of fault regimes. This study provides an in-depth observation of vertical stress prediction utilizing numerous approaches using the Techlog 2015 software. Gardner's method results in incorrect vertical stress values with a problem that this method doesn't start from the surface and instead relies only on sound log data. Whereas the Amoco, Wendt non-acoustic, Traugott, average technique simply needed density log as input and used a straight line as the observed density, this was incorrect for vertical computing stress. The results of these methods

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sat Aug 01 2015
Journal Name
International Journal Of Computer Science And Mobile Computing
Image Compression based on Non-Linear Polynomial Prediction Model
...Show More Authors

Publication Date
Tue Jul 01 2025
Journal Name
Iraqi Journal Of Hematology
The role of CD319, CD117, CD28, CD49e, CD56, and CD44 expression as diagnostic and prognostic markers in multiple myeloma
...Show More Authors

BACKGROUND Multiple myeloma (MM) is a plasma cell disorder characterized by the infiltration of clonal plasma cells in the bone marrow and the detection of a monoclonal immunoglobulin in serum and/or urine. Renal failure, anemia, hypercalcemia, and the presence of bone lesions are the hallmarks of the disease. The study aimed to evaluate the clinical, hematological, radiological, and immunophenotypic features of MM patients and to identify prognostic factors influencing survival outcomes. This cohort study included 77 newly diagnosed, untreated MM patients. Their clinical presentation, laboratory data, imaging results, and the expression of flow cytometry markers were analyzed in correlation with the 1-year overall survival (OS). The mean a

... Show More
View Publication Preview PDF
Clarivate Crossref
Publication Date
Thu Dec 15 2022
Journal Name
Al-academy
The art of adornment and make-up in the ancient civilizations of Mesopotamia and the old country of Yemen as a model
...Show More Authors

This research sheds light on those discrepancies in the use of ornaments, adornment and perfumes, as well as the art of cosmetics, in two important civilizations, namely, the Mesopotamian civilization as the earlier civilization, and the civilization of Yemen, which represents the first Arab civilization. Through the foregoing, our research includes two topics, the first topic included the history of the use of decorations, ornaments and perfumes in the civilization of Mesopotamia, while the second topic included the study of ornaments, adornment and cosmetic art in the ancient civilization of Yemen. And then the research came out with a number of conclusions that the researcher considers very important to highlight the differences and f

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Nov 01 2016
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
Loranthus europaeus as an alternative medicine in treatment of acute cutaneous Lesihmaniasis
...Show More Authors

KE Sharquie, AA Noaimi, BA Saleh, Journal of Cosmetics, Dermatological Sciences and Applications, 2016 - Cited by 15

View Publication