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 Jun 01 2007
Journal Name
Journal Of The College Of Languages (jcl)
Old Age as a Motif In the Poetry of W.B. Yeats (1865-1939)
...Show More Authors

In 1908 , the American poet Ezra Pound (1885-1972) , the central figure in the modern movement who was the driving force behind several movements , notably Imagism and Vorticism , met the Irish poet W. B. Yeats in London . Pound was employed as his secretary and the two soon became close friends . He found Yeats a realist, symbolist and a metaphysical poet with an uncanny power over words and regarded him the greatest living poet .The poetical style and the occult beliefs of the Irish poet drew the attention of the American Imagist .During the war, Pound and Yeats lived together at Stone Cottage in Sussex studying Japanese literature .Speaking of Yeats , T. S. Eliot described him as "one of those few whose history is the history of their

... Show More
View Publication Preview PDF
Publication Date
Thu Mar 07 2024
Journal Name
Problems Of Endocrinology
KI-67 as a predictive indicator of papillary thyroid cancer in Iraqi patients
...Show More Authors

BACKGROUND. KI-67 (MKI-67 in humans) is a protein able to bind to DNA which contributes to cell growth and cell proliferation. KI-67 is currently considered as a biomarker that is widely utilized as prognostic indicator for evaluating cell proliferation, diagnosing diseases, and conducting research. Several different kinds of cancer have high Ki-67 expression, which simplifying the choice of treatment for individuals with various cancer types.AIM. The objective was to evaluate the expression of KI67 in patients suffering papillary thyroid cancer (PTC) also the association between patients age and gender and KI67 expression.MATERIALS AND METHODS. To undertake an in-

... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Thu Mar 01 2018
Journal Name
Asian Journal Of Multidisciplinary Studies
Entrepreneurial mindset and aspiration as critical success factor for small business performance in Iraq
...Show More Authors

The aim of this research is to examine the relationship between entrepreneurial mindset and aspiration and small business performance Baghdad, Iraq. This study proposed a quantitative analysis in which entrepreneurial mindset and aspiration is a critical success factor of small business in Iraq. The method employed in the collection of data was by the means of self-administered questionnaire which was filled and completed by small business owners randomly selected from a sampling frame of registered small businesses. The questionnaire was adapted from the study of Davis, Halls & Mayer (2015) and Abdel-Maksoud, Asada & Nakagawa (2008) which was used to measure entrepreneurial mindset and aspiration using a ten items scale and small business

... Show More
Publication Date
Sun Mar 12 2017
Journal Name
Al-academy
Presence and Absence in the Iraqi Theatre Performance: Summer's Rain Play as an Example
...Show More Authors

The presence and absence binary is an essential part of and a motivation for the direction vision which depends on the principle that the components of the theatre performance move in contrast with each other; one is directly informative which is the presence relations and the other is structural that is identical to the absence relations. The first is material band visual that evokes the incorporeal mental absent. Hence, the present study(Presence and Absence in the Iraqi Theatre Performance :Summer's Rain Play as an Example) aims at explaining those relations and their transformations between presence and absence in the performance

View Publication Preview PDF
Crossref
Publication Date
Thu Dec 31 2020
Journal Name
Political Sciences Journal
Russian-American competition in the Middle East:Power and roles conflict: Syria as a model
...Show More Authors

Because of its importance in the world, Middle East area is one of the competition areas between the major and great powers. Among those powers are Russia and United states of America. The competition between these two powers to control Syria is greatly clear since 2011. It is also one of the most important subject in the international politics. This importance comes from the importance of Russia and the United States of America besides importance of the Middle East. At the end of the cold war, United States of America maintained its role in the international system and became the only pole that dominated the international affairs while Russia tried to overcome the challenges inherited from the former Soviet Union, and it succeeded in th

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Apr 30 2023
Journal Name
Al-kindy College Medical Journal
Serum Myelin Oligodendrocyte Glycoprotein and Myelin Protein Zero as Diagnostic Biomarkers in Diabetic Neuropathy
...Show More Authors

Background: Diabetic neuropathy can affect any peripheral nerve, including sensory neurons, motor neurons, and the autonomic nervous system. Therefore, diabetic neuropathy has the potential to affect essentially any organ and can affect parts of the nervous system like the optic nerve, spinal cord, and brain. In addition, chronic hyperglycemia affects Schwann cells, and more severe patterns of diabetic neuropathy in humans involve demyelization. Schwann cell destruction might cause a number of changes in the axon. study aims to evaluate serum myelin protein level as a predicting marker in the diagnosis of diabetic neuropathy and to prevent early neuropathy complications of type 2 diabetes.

Sub

... Show More
View Publication Preview PDF
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Mon Jun 05 2023
Journal Name
Journal Of Engineering
Prediction of Compressive Strength of Reinforced Concrete Structural Elements by Using Combined Non-Destructive Tests
...Show More Authors

This research is devoted to investigate relationship between both Ultrasonic Pulse Velocity and Rebound Number (Hammer Test) with cube compressive strength and also to study the effect of steel reinforcement on these relationships.
A study was carried out on 32 scale model reinforced concrete elements. Non destructive testing campaign (mainly ultrasonic and rebound hammer tests) made on the same elements. About 72 concrete cubes (15 X 15 X15) were taken from the concrete mixes to check the compressive strength.. Data analyzed.Include the possible correlations between non destructive testing (NDT) and compressive strength (DT) Statistical approach is used for this purpose. A new relationships obtained from correlations results is give

... Show More
View Publication Preview PDF
Crossref (7)
Crossref
Publication Date
Tue Jun 27 2023
Journal Name
Journal Of Global Innovations In Agricultural Sciences
The use of remote sensing technology in defining the water depth in the lakes and water bodies: Western Iraq as a case study
...Show More Authors

The study's primary purpose is to explore an appropriate way of monitoring and assessing water depths using the satellite remote sensing technique of the Al Habbaniyah Lake in Iraq. This research studied the experience-conditions (thresholds) of different bands for multi-temporal satellite image data with different satellite image sensors (Landsat 5-TM, and EO1-ALI) for the same region, to recognize regions of water depths. The threshold values are taken that to separate the Al Habbaniyah Lake to the required depths (shallow, deep, and very deep), as a supervised method. A three-dimension feature space plot had used to represent these regions. The relationship of the mean values of the three separated water regions with all TM and A

... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Fri Jan 01 2016
Journal Name
Journal Of The College Of Languages (jcl)
Linguistic contast between bilateral and trilateral roots in Semitics languages (Arabic and Syriac as a model)
...Show More Authors

The present study investigates the relation between the biliteral and triliteral roots which is the introduction to comprehend the nature of the Semitic roots during its early stage of development being unconfirmed to a single pattern. The present research is not meant to decide on the question of the biliteral roots in the Semitic languages, rather it is meant to confirm the predominance of the triliteral roots on these languages which refers, partially, to analogy adopted by the majority of linguists. This tendency is frequently seen in the languages which incline to over generalize the triliteral phenomenon, i. e., to transfer the biliteral roots to the triliteral room, that is, to subject it to the predominant pattern regarding the r

... Show More
View Publication Preview PDF
Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Advanced Pharmacy Education And Research
Formulation and evaluation of mucoadhesive buccal tablet of Anastrozole
...Show More Authors

View Publication Preview PDF
Scopus (7)
Crossref (6)
Scopus Crossref