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 11 2025
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of Remineralizing Toothpastes on Enamel Surface Roughness after Hybrid Laser Bleaching (An In vitro Study)
...Show More Authors

Background: one of the complications of power bleaching is surface roughness of enamel which increases the possibility of post bleaching teeth discoloration. The aim of the present study is to evaluate the effect of toothpaste containing nano hydroxyapatite, NovaMin and kin sense fluoride on surface roughness of human tooth enamel after laser bleaching with 35% hydrogen peroxide bleaching gel. Materials and Methods: Twenty human enamel incisors were cleaned and their labial surface polished up to #1200, then categorized into four equal groups; first group kept without bleaching as a control group, while the remaining three experimental groups were bleached with 35% hydrogen peroxide, and each group treated with a restore paste containing o

... Show More
View Publication Preview PDF
Publication Date
Wed Dec 15 2010
Journal Name
Iraqi Journal Of Laser
Photo Response of Locally Isolated Methicillin-Resistant Staphylococcus aureus to Q-switched Nd:YAG Laser In Vitro Study
...Show More Authors

This prospective study investigates the prevalence of methicillin-resistant S.aureus (MRSA)
in burn unit of Al-Kindy Iraqi hospital, their susceptibility to antibiotics and bactericidal effect of near
infrared light from high powered 1064nm Nd: YAG laser and green light 532nm from SHG Nd: YAG laser
using various energy densities on these bacteria. Twenty four clinical isolates of S.aureus out of sixty
four examined patients with sever burn ulcers.MRSA was associated with 50% of S.aureus infections
.Results of antimicrobial susceptibility revealed that MRSA were multidrug resistant. After laser treatment
of non MRSA with Nd:YAG with wavelength of 1.064nm, 4mm beam diameter, energy density of
0.636 kh/cm2 and 180sec ex

... Show More
View Publication Preview PDF
Publication Date
Thu Oct 31 2013
Journal Name
Al-khwarizmi Engineering Journal
Simulation of a Wet Sulfuric Acid Process (WSA) for Utilization of Acid Gas Separated from Omani Natural Gas
...Show More Authors

In this study, a proposed process for the utilization of hydrogen sulphide separated with other gases from omani natural gas for the production of sulphuric acid by wet sulphuric acid process (WSA) was studied. The processwas simulated at an acid gas feed flow of   5000 m3/hr using Aspen ONE- V7.1-HYSYS software. A sensitivity analysis was conducted to determine the optimum conditions for the operation of plant. This included primarily the threepacked bed reactors connected in series for the production of sulphur trioxidewhich represented the bottleneck of the process. The optimum feed temperature  and catalyst bed volume for each reactor were estimated and then used in the simulation of the whole process for tw

... Show More
View Publication Preview PDF
Publication Date
Mon Sep 01 2014
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci
Studying the Biological Activity of Some Oxazepine Derivatives Against Some G(+) and G(-) Bacteria.
...Show More Authors

The preliminary test of the compounds N [2– (3,4–dimethoxy nitrobenzene oxazepine– 2,3–dihydro–4,7–dione]–5–mercupto–2–amino–1,3,4–thiadiazol [A] and N [ 2–anthralidene– 5– ( 2–nitrophenyl ) –1,3–oxazepine–4,7–dione–2–d](5–mercapto–1,3,4–thiadiazole–2–amin) [B] , showed that they possess high activity against some positive and negative bacteria , like pseudomonas aeruginosa (pseudo.), Escherichia coli (E-coli), staphylococcus aureus (sta.) and Bacillus subtilis (Ba.) and finally there is a study of the effect of some antibiotics like streptomycin (S), gentamycin (GN), chloramphenicol (C) and Nalitixic acid (NA) in order to compare the differences in effects. In the present study, results

... Show More
Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Studying the Biological Activity of Some Oxazepine Derivatives Against Some G(+) and G(-) Bacteria
...Show More Authors

  The preliminary test of the compounds N [2– (3,4–dimethoxy nitrobenzene oxazepine– 2,3–dihydro–4,7–dione]–5–mercupto–2–amino–1,3,4–thiadiazol [A] and N [ 2–anthralidene– 5– ( 2–nitrophenyl ) –1,3–oxazepine–4,7–dione–2–d](5–mercapto–1,3,4–thiadiazole–2–amin) [B] , showed that they possess high activity against some positive and negative bacteria , like pseudomonas aeruginosa (pseudo.), Escherichia coli (E-coli), staphylococcus aureus (sta.) and Bacillus subtilis (Ba.) and finally there is a study of the effect of some antibiotics like streptomyci

... Show More
View Publication Preview PDF
Publication Date
Wed Dec 18 2019
Journal Name
Baghdad Science Journal
A Modified Approach by Using Prediction to Build a Best Threshold in ARX Model with Practical Application
...Show More Authors

The proposal of nonlinear models is one of the most important methods in time series analysis, which has a wide potential for predicting various phenomena, including physical, engineering and economic, by studying the characteristics of random disturbances in order to arrive at accurate predictions.

In this, the autoregressive model with exogenous variable was built using a threshold as the first method, using two proposed approaches that were used to determine the best cutting point of [the predictability forward (forecasting) and the predictability in the time series (prediction), through the threshold point indicator]. B-J seasonal models are used as a second method based on the principle of the two proposed approaches in dete

... Show More
View Publication Preview PDF
Scopus (1)
Scopus Clarivate Crossref
Publication Date
Wed Sep 01 2021
Journal Name
Https://www.researchgate.net/journal/university-of-baghdad-engineering-journal-1726-4073
Evaluation of Drinking Water Quality in Al Wahda Treatment Plant in Baghdad City- Iraq
...Show More Authors

This study aims to evaluate drinking water quality at the Al Wahda plant (WTP) in Baghdad city. A conventional water treatment plant with an average flow rate of 72.82 MLD. Water samples were taken from the influent and effluent of the treatment plant and analyzed for some physicochemical and biological parameters during the period from June to November 2020. The results of the evaluation indicate that treated water has almost the same characteristics as raw water; in other terms, the plant units do not remove pollutants as efficiently as intended. Based on this, the station appears to be nothing more than a series of water passage units. However, apart from Total dissolved solids, the mean values of all parameters in the study were

... Show More
Crossref (1)
Crossref
Publication Date
Tue Aug 07 2018
Journal Name
Indian Journal Of Natural Sciences
Evaluation of Drinking Water Quality in Al Wathba Treatment Plant in Baghdad City-Iraq
...Show More Authors

Publication Date
Wed Sep 01 2021
Journal Name
Journal Of Engineering
Evaluation of Drinking Water Quality in Al Wahda Treatment Plant in Baghdad City- Iraq
...Show More Authors

This study aims to evaluate drinking water quality at the Al Wahda plant (WTP) in Baghdad city. A conventional water treatment plant with an average flow rate of 72.82 MLD. Water samples were taken from the influent and effluent of the treatment plant and analyzed for some physicochemical and biological parameters during the period from June to November 2020. The results of the evaluation indicate that treated water has almost the same characteristics as raw water; in other terms, the plant units do not remove pollutants as efficiently as intended. Based on this, the station appears to be nothing more than a series of water passage units. However, apart from Total dissolved solids, the mean values of all parameters in th

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Jun 01 2021
Journal Name
The Journal Of Continuing Education In Nursing
Debate as a Teaching Strategy in Nursing
...Show More Authors

Debate is a teaching strategy in nursing education that enhances students' critical thinking. Although debate can be an effective teaching strategy, it is not without limitations. This article discusses the advantages and disadvantages of debate as a teaching strategy in nursing. Also, evaluating debates and choosing topics are highlighted. [ J Contin Educ Nurs . 2021;52(6):263–265.]

View Publication
Scopus (1)
Crossref (2)
Scopus Clarivate Crossref