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 Jul 01 2020
Journal Name
Journal Of Physics: Conference Series
A New Iterative Methods For a Family of Asymptotically Severe Mappings
...Show More Authors
Abstract<p>The aim of this paper is to introduce the concepts of asymptotically p-contractive and asymptotically severe accretive mappings. Also, we give an iterative methods (two step-three step) for finite family of asymptotically p-contractive and asymptotically severe accretive mappings to solve types of equations.</p>
View Publication
Scopus (6)
Crossref (2)
Scopus Crossref
Publication Date
Sun Dec 07 2014
Journal Name
Baghdad Science Journal
Study the Changes of Thyroid Hormones Levels Following Major Urological Surgery
...Show More Authors

This study was designed to evaluate the effect of major surgery on thyroid hormones and thyrotropin in patient undergoing major lower abdominal surgery. The study included fifty patients scheduled for elective major lower abdominal surgery, the serum levels of T3, T4 and TSH were determined one day preoperatively, intraoperative, one day postoperatively, two days postoperatively, and rT3 was determined one day preoperatively, and one day postoperatively. We observed that the levels of (T3, T4, TSH) increased significantly (P<0.05) intraoperatively, one day postoperatively the levels of T3 and T4 reduced significantly (P<0.05), while TSH reduced not significantly (P>0.05), and two days postoperatively T4 and TSH returned to increase si

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Apr 01 2015
Journal Name
2015 Annual Ieee Systems Conference (syscon) Proceedings
Automatic generation of fuzzy classification rules using granulation-based adaptive clustering
...Show More Authors

View Publication
Scopus (4)
Crossref (4)
Scopus Crossref
Publication Date
Thu Oct 15 2015
Journal Name
Journal Of Physical Vapor Deposition Science And Technology (jpvdst)
Physical Properties of Nanostructured Silicon Dioxide Prepared by Pulsed-Laser Deposition
...Show More Authors

Publication Date
Sat Jul 25 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Surface area measurements of upper dental cast with different final impressionss
...Show More Authors

Background : surface area anatomy is a proportional point to the retention of complete denture, in past there was no quantitative method to evaluate the surface area, nowadays the size and shape of maxillary arch is measured by different electronically and mathematical devices. A study was therefore, undertaken to measure surface area of upper dental cast that was taken by different final impressions. Materials and methods: twenty patients were examined. All of them had a healthy palate with no singe of injury, trauma, or deformity. Casts were taken by three different final impressions; zinc oxide, additional silicon, and poly ether. And two different devices were used; the computerized one and the Aluminum foil measure. Age, se

... Show More
View Publication Preview PDF
Publication Date
Sat Nov 07 2020
Journal Name
Theory And Practice Of Mathematics And Computer Science
Discussion on Bipolar Fuzzy n-fold KU-ideal of KU-algebras
...Show More Authors

Publication Date
Sat Jul 25 2026
Journal Name
Journal Of Techniques
RESPONSE OF AWASSI SHEEP TO FREQUENT LAMBING UNDER PRIVATE FARM CONDITION
...Show More Authors

View Publication
Publication Date
Wed May 10 2023
Journal Name
Journal Of Engineering
ANALYTICAL SOLUTION OF UNSATURATED SOIL WATER FLOW FROM A POINT SOURCE
...Show More Authors

Water flow into unsaturated porous media is governed by the Richards’ partial differential equation expressing the mass conservation and Darcy’s laws. The Richards’ equation may be written in three forms,where the dependent variable is pressure head or moisture content, and the constitutive relationships between water content and pressure head allow for conversion of one form into the other. In the present paper, the “moisture-based" form of Richards’ equation is linearized by applying Kirchhoff’s transformation, which
combines the soil water diffusivity and soil water content. Then the similarity method is used to obtain the analytical solution of wetting front position. This exact solution is obtained by means of Lie’s

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Wed Dec 30 2015
Journal Name
College Of Islamic Sciences
The concept of sohba when the Golden Imam Through his books
...Show More Authors

Scientists were interested in the statement of the concept of companions and the definition of the companion in terms of his status or his novel or inherent to the Prophet of Allah (peace be upon him) and was for those who did not walk in the translations and the abundant share in this work, and among these scientists Hafiz Shams al-Din al-Dhahabi, which was translated to the companions His books, indicating their status and effort, and who had a novel of them - what we will see in the folds of the research, God willing -

View Publication Preview PDF
Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
An Extended Subclass of Meromorphic Multivalent Functions Involving Ruscheweyh Derivative Operator
...Show More Authors

     In this paper, we introduce and discuss an extended subclass〖 Ą〗_p^*(λ,α,γ) of meromorphic multivalent functions involving Ruscheweyh derivative operator. Coefficients inequality, distortion theorems, closure theorem for this subclass are obtained.

View Publication
Scopus Crossref