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 2012
Journal Name
Journal Of Economics And Administrative Sciences
The Effect of the Stability of Some Commodity Activities in Iraq on the Estimation of the Statistical Data Models for the Period (1988-2000)
...Show More Authors

There is an assumption implicit but fundamental theory behind the decline by the time series used in the estimate, namely that the time series has a sleep feature Stationary or the language of Engle Gernger chains are integrated level zero, which indicated by I (0). It is well known, for example, tables of t-statistic is designed primarily to deal with the results of the regression that uses static strings. This assumption has been previously treated as an axiom the mid-seventies, where researchers are conducting studies of applied without taking into account the properties of time series used prior to the assessment, was to accept the results of these tests Bmanueh and delivery capabilities based on the applicability of the theo

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Oct 01 2009
Journal Name
Jssdds
Topical 10% lactic acid solution in the treatment of pityriasis versicolor in comparison with topical 1% clotrimazol solution (single-blind, comparative and therapeutic study)
...Show More Authors

KE Sharquie, AA Noaimi, AM Oweid, JSSDDS, 2009 - Cited by 2

View Publication
Publication Date
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
Study of the Anticancer and Antimicrobial Biological Activity of a New Series of Thiohydantoin Derivatives
...Show More Authors

        Recently, some prostate cancer patients have acquired resistance to the second -generation drugs (anzalutamide and apalutamide) prescribed for the treatment of this disease due to the emergence of the F876L mutation, which represents a challenge to modern medicine. In this study, a new series of 2-thiohydantoin derivatives were prepared through the reaction of different derivatives of maleimide (1c-4c) with isothiocyanate derivatives. The prepared compounds were diagnosed using FT-IR,1H-NMR ,13C-NMR, Mass spectra. The prepared series compounds has been studied against prostate cancer cells. The MTT assay was used to determine the activity of the prepared compounds against prostate cancer cells. The da

... Show More
View Publication Preview PDF
Scopus (2)
Scopus Crossref
Publication Date
Tue Aug 22 2023
Journal Name
Microbial Science Archives
Unveiling Westiellopsis akinetica: a novel species in the Iraqi habitat, and contrasting its distinctive attributes with Westiellopsis prolifica
...Show More Authors

This is the first record of a new species of cyanobacteria Westiellopsis akinetica in the Iraqi environment, Samples were collected on June 2013 and the existence of it was not documented before. We isolated and purified this species ten years ago in Iraq, but we couldn't identify accurately based on all taxonomic handbooks. This is due to the species features being different from the other documented species in the available taxonomic lectures. It resembled many species by morphological characteristics such as Fischerella muscicola, Fischerella thermalis, Westiellopsis biateralis SA16. Westiellopsis interrupta, Westiellopsis persica SA33, Westiellopsis prolifica and Symphyonema bifilamentata. Describing a new species of the Westiellops

... Show More
View Publication
Crossref
Publication Date
Sun Jan 01 2023
Journal Name
The Egyptian Journal Of Hospital Medicine
Changes in Interleukin-35 (IL-35), Anti-TSHR antibody and Human Insulin- like Growth Factor 1 Receptor (IGF1R) in Graves’ Disease Patients Treatedwith Radioactive Iodine
...Show More Authors

View Publication
Crossref
Publication Date
Tue Dec 06 2022
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Blended Learning in Nursing Education at the Middle Region in Iraq
...Show More Authors

Abstract

Objective(s): To evaluate blended learning in nursing education at the Middle Region in Iraq.

Methodology: A descriptive study, using evaluation approach, is conducted to evaluate blended learning in nursing education in Middle Region in Iraq from September 26th, 2021 to March 22nd, 2022. The study is carried out at two Colleges of Nursing at the University of Baghdad and University of Tikrit in Iraq. A convenient, non-probability, sample of (60) undergraduate nursing students is selected. The sample is comprised of (30) student from each college of nursing, Self-report questionnaire is constructed from the literature, for e

... Show More
View Publication Preview PDF
Publication Date
Thu Jun 30 2016
Journal Name
Al-kindy College Medical Journal
Evaluation Of Risk Factors In Perforated Acute Appendicitis In Al-Kindy Teaching Hospital
...Show More Authors

Background: Appendectomy is still one of the most commonly performed emergency surgical procedures worldwide.Avoiding delays in the diagnosis in these patients may play a role in reducing observed morbidity.Aim of study:To analyze the clinico-pathological profile and outcomes of patients undergoing emergency appendectomies to determine risk factors influencingcomplicaions.Type of the study: A prospective analytic studyPatients and Methods: The study involves 108 patients underwent emergency appendectomies at Al-kindy teaching hospital from April 2014 to March 2015. Appendicitis was categorized into two groups perforated andnonperforatedappendicities. A comparison between them was made in regard to Gender, Age, clinical presentation, inve

... Show More
View Publication Preview PDF
Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Different Concentrations of Melatonin on the Time-course of Nitrite–induced Oxidation of Hemoglobin: In vitro Study
...Show More Authors

         Melatonin is a potent scavenger of reactive oxygen species or free radicals like superoxide and hydroxyl radicals. The oxidation of hemoglobin to methemoglobin (meth-Hb) by oxidizing compounds has been widely studied. The present work was designed to evaluate the ability of different concentrations of melatonin to inhibit nitrite–induced oxidation of hemoglobin. Blood samples were obtained from apparently healthy individuals from which erythrocyte hemolysate was prepared. Different concentrations of melatonin (10-9-1.0 mg/ml) were incubated for 10 min with the hemolysate, then to the resultant mixture 1 ml of sodium nitrite (final concentration 0.6 mM) was added, and the

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue May 16 2023
Journal Name
Political Sciences Journal
The Dens of Extremism and Terrorism in Syrian Camps (Al-Hol as a model)
...Show More Authors

 

After the defeat of the military terrorist organization "ISIS" and the fall of the throne of its alleged state in the Iraqi city of Nineveh, in Syrian Baghouz, and the end of its control over the land, the Syrian camps, especially "Al-Hol" camp, emerge as an incubator for the ideology of the terrorist organization "ISIS" and a vital base for its consolidation and dissemination, which includes (68,000- 73,000) people. During the years following the military defeat of (ISIS), the camp witnesses the spread of extremist ideas widely at the hands of its residents, including the families of the organizations dead's, extremist detainees, and those who deal with it, taking advantage of the deterioration of the environmental, se

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Oct 26 2018
Journal Name
Journal Of Planner And Development
Acceptable and Unacceptable Growth of Industrial Agglomeration in Urban Environment. Baghdad as Case Study
...Show More Authors

View Publication Preview PDF