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
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
...Show More Authors

The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Mon Apr 10 2017
Journal Name
Al-mustansiriyah Journal Of Science
Synthesis, characterization and antibacterial Evaluation for mixed-ligand Complexes of Nickle (II), Manganese(II), Copper( II),Cobalt(II) and Mercury(II) with Tetradentate Schiff base and 1,10-phenanthroline
...Show More Authors

An abstract is a brief summary of a research article, thesis, Schiff base ligand (L) was prepared by the reaction of 4-aminantipyrine with o-phenylenediamine, the prepared ligand characterized by Micro elemental Analysis, FT. IR, UV-Vis, and 1H,13C-NMR spectroscopy.complexes of Mn(II), Co(II), Ni(II), Cu(II) and Hg(II) with Schiff base and 1,10-phenanthroline (Phen) have been investigated in aqueous ethanol with (1:1:1) (M:L:Phen). The prepared complexes were characterized using flame atomic absorption, (C. H. N) Analysis, FT. IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. From the obtained data the octahedral structure was suggested for all complexes. The biological screening effects o

... Show More
Publication Date
Tue Dec 06 2022
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Nurses' Attitudes towards Patients’ End of life in Diyala Governorate
...Show More Authors

Abstract:

Objectives: To assess nurses' attitude toward end of life phase. To find out  relationships between nurses attitude and socio demographic data (age, gender, level of education, years of experience).

Methodology: A descriptive cross-sectional study design is carried out to assess the attitude on nurses concerning patient at the end of life phase at critical care units, from the period of (1nd November 2021) to (1th February 2022). A probability sample random sampling technique used. Then, the number of participants in Baquba Teaching Hospital and general al khalis hospital were determined by using rando

... Show More
View Publication Preview PDF
Publication Date
Mon Jun 30 2014
Journal Name
Al-kindy College Medical Journal
Evaluation of D-Dimer in the diagnosis of suspected deep vein thrombosis
...Show More Authors

Background: Deep vein thrombosis is a multi causal disease and its one of most common venous disorder, but only one quarter of the patients who have signs and symptoms of a clot in the vein actually have thrombosis and need treatment .The disease can be difficult to diagnose. Venous ultrasound in combination with clinical finding is accurate for venous thromboembolism, its costly because a large number of patients with suspicious signs and symptoms. Venography still the gold standard for venous thromboembolism but it is invasive. The D-dimer increasingly is being seen as valuable tool rolling out venous thromboembolism and sparing low risk patients for further workup.Objectives: this study has designed the role of D-dimer to confirm diag

... Show More
View Publication Preview PDF
Publication Date
Wed Mar 01 2017
Journal Name
Photodiagnosis And Photodynamic Therapy
Photodynamic therapy in the management of actinic keratosis: Retrospective evaluation of outcome
...Show More Authors

View Publication Preview PDF
Scopus (20)
Crossref (18)
Scopus Clarivate Crossref
Publication Date
Wed Dec 12 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Quality of Life for Secondary School Students in Kirkuk City
...Show More Authors

Objective(s):To evaluate the quality of life among secondary and to find out the relationship between students'quality of life and their socio-demographic characteristics of age, gender, residence, marital status, father's and mother's education, and family financial status in Kirkuk City. Methodology: A cross-sectional study is conducted on (100) studentwho are boys and girls aged(13 to 24) years old. These subjects are studying at secondary schools in Kirkuk City.The study is carried out at secondary schools in Kirkuk City from 7th July 7th 2014 to May 7th 2015. A questionnaire is constructed for the purpose

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 09 2018
Journal Name
Baghdad Science Journal
Evaluation of the Ecosystem Services of the Central Marsh in Southern Iraq
...Show More Authors

Ecosystems provide humans with services that include benefits from food, fresh water, climate regulation, and socio-economic assets. The Mesopotamian marshlands are among the largest wetlands in the Middle East and they provide various benefits. However, ecosystem services of the Marshlands are consistently undervalued in national economic analysis and decision making. This study focusses on the Central Marshes, the first National Park in Iraq, and is the first attempt at valuing a series of ecosystem services from a valuable natural ecosystem in Iraq. We adopted the Toolkit for Ecosystem Services Site-Based Assessment (TESSA) for the determination of biophysical and economic values of services at the site level. Data on key ecosystem se

... Show More
View Publication Preview PDF
Scopus (9)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Wed Mar 30 2016
Journal Name
College Of Islamic Sciences
The conversations of reason and thinking as stated in the Sunnah and its impact on human behavior
...Show More Authors

The Sunnah of the Prophet has a great impact in building human behavior, and the formation of Islamic thought, has worked to spread science in all of Egypt, as it carried to the people of the eternal prophecy of the love of science, it was a source of knowledge and civilization. It is a generous source, a rich source of the Islamic nation, always tender, and renewed benefit, which is not only a source of legislation and language but is a source of guidance for thought and guidance of behavior, and the Hadith The importance is obvious In the integration of Islam, and show aspects of human integration in the personality of Mustafa , and the Muslims are interested in talking - collected and codification -, and made the effort of the cent

... Show More
View Publication Preview PDF
Publication Date
Thu Jun 01 2017
Journal Name
Journal Of The College Of Languages (jcl)
Alice walker as an Activist and celebrator of Resistance in Meridian (1976) and The Color Purple (1982).
...Show More Authors

    Alice Walker (1944) ranks among the greatest American writers of the twentieth century. Through her novels Meridian and the color Purple, Alice outlines many issues concerning the effect of authoritarian thinking upon its often innocent victims, and the possibility of meaningful, productive resistance. Walker's texts aim at giving a voice to those who have no voice especially those poor, rural black women who are robbed of power and the right to make decisions about their own lives by a range of forces standing against them. These texts also aim at clarifying how Walker's female protagonists, Meridian and Celia try to free themselves from oppression, misery , fear and underestimation

... Show More
View Publication Preview PDF
Publication Date
Mon Feb 16 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Andrews' six keys of normal occlusion in a sample of Iraqi adults in Baghdad city
...Show More Authors

Background: The Andrews’ six keys of normal occlusion contribute individually and collectively to the total scheme of occlusion and, therefore, are viewed as essential to successful orthodontic treatment. The present research aims to evaluate the presence of the parameters of the Andrews’ Six Keys of normal occlusion in a sample of 100 Iraqi adults with complete permanent dentition and clinically acceptable normal occlusion (Angle’s Class I) in Baghdad city. Their age range 18-25 years (60 males and 40 females). Materials and methods: Each patient was subjected to clinical examination and then study cast models were made, with their occlusal records. The measuring tools that have been used involved: Three-dimensional goniometer to me

... Show More
View Publication Preview PDF