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
Sat Dec 31 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Corrosion Inhibition of Carbon Steel in Hydrochloric Acid under Dynamic Conditions
...Show More Authors

In this work, studying the effect of ethylenediamine as a corrosion inhibitor was investigated for carbon steel in aerated HCl solution in range of 0.1-1N under dynamic conditions, i.e., rotational velocity of 400–1200 rpm in the temperature range 35 – 65 ºC.  Weight loss method was employed in absence and presence of the inhibitor as an adsorption type in concentration range 1000 – 5000 ppm using rotating cylinder specimens. The experimental results showed that corrosion rate in absence and presence of inhibitor is increased with increasing temperature, rotational velocity and concentration of acid. It is decreased with increasing inhibitor concentration for the whole range of temperature, rotational velocity and concentrati

... Show More
View Publication Preview PDF
Publication Date
Sun Sep 30 2007
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Electrochemical Behavior of Chemical Conversion Coated Aluminum ASA6061 in Chromic Acid
...Show More Authors

The corrosion behavior of bare and chemical conversion coated (through anodizing) aluminum ASA 606 I in stagnant chromic acid solutions . Solutions of 2, 6 & J O wt. % Cr03 at 45°C, have been investigated using polarization technique. The anodizing experiments were conducted under fixed conditions of 35 minute exposure time and 30 volt supplied voltage. The most important feature achieved was the great difference in behavior between the anodic polarization curves for bare and anodized aluminum in different concentrations of chromic acid solutions.

View Publication Preview PDF
Publication Date
Sun Oct 01 2023
Journal Name
Journal Of Medicine And Life
Evaluating the effect of ursodeoxycholic acid (UDCA) in comparison with dexamethasone and diclofenac in a rat model of rheumatoid arthritis
...Show More Authors

View Publication
Scopus (4)
Crossref (4)
Scopus Crossref
Publication Date
Fri Oct 01 2010
Journal Name
Iraqi Journal Of Physics
Evaluation of polyurethane and polyurethane /polyvinyl chloride blend coatings on steel as corrosion protection using EIS technique
...Show More Authors

This paper was aimed to evaluate the polyurethane (PU) and polyurethane/polyvinyl chloride (90 wt. % / 10 wt. %) as organic coating of carbon steel substrate against marine environment (3.5 wt.% NaCl aqueous solution) as a severe corrosion environment . The electrochemical impedance spectroscopy (EIS) and fitting impedance data by ZsimpWin 3.22 software were used to estimate the physical barrier of the samples for different exposure times. Different equivalent electrical circuits were proposed for the physical barrier at different immersion times to get appropriate fitting .Both PU and PU/PVC coatings showed excellent corrosion protection ability for steel .The PU/PVC coating showed better protection and stability than PU coating against

... Show More
View Publication Preview PDF
Publication Date
Wed May 10 2023
Journal Name
Journal Of Planner And Development
Analysis and evaluation of related factors affecting community Participation as a policy to upgrade residential slums area
...Show More Authors

have suffered from deteriorating residential neighborhoods, poor economic, social and urban living conditions of the population and deteriorating the infrastructural and superior services. These problems were the secretions of these cities' rapid urbanization. Based on the principles of sustainable urban planning and in order to achieve adequate opportunities for the lives of the population and provide them with sustainable livelihoods, policies have emerged to upgrade along the lines of community participation and programmes to reform and develop those neighbourhoods, raise their efficiency and make them livable. Thus, the problem of research was identified "The absence of a comprehensive cognitive perception of the most prominent facto

... Show More
View Publication Preview PDF
Publication Date
Tue Aug 05 2014
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
FORMULATION AND EVALUATION OF FLOATING ORAL IN-SITU GEL OF METRONIDAZOLE
...Show More Authors

View Publication Preview PDF
Scopus (20)
Scopus
Publication Date
Fri Sep 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of alpha amylase and peroxidase in saliva of pregnant women
...Show More Authors

Background: Pregnancy is a natural physiological state that involves several biochemical modifications. Saliva is consisted of many types of proteins such as salivary alpha amylase and salivary peroxidase that might be affected by pregnancy. The former enzyme is considered one of the most prevalent proteins that is released by highly differentiated epithelial acinar cells and has been shown to have enzymatic activities while the latter has been approved that it  has a significant role in oral health. The purpose of this study was to the evaluate the salivary levels of alpha-amylase and peroxidase in pregnant and non-pregnant women. Materials and Methods: Sixty pregnant women were grouped according to the pregnancy trimesters. The first

... Show More
View Publication Preview PDF
Scopus (2)
Crossref (4)
Scopus Crossref
Publication Date
Sun Jan 01 2023
Journal Name
Journal Of Advanced Pharmaceutical Technology & Research
Use of factorial design in formulation and evaluation of intrarectal in situ gel of sumatriptan
...Show More Authors

View Publication
Scopus (18)
Crossref (14)
Scopus Clarivate Crossref
Publication Date
Fri Jun 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Histological and histomorphometric studies of the effects of hyaluronic acid on osseointegration of titanium implant in rabbits
...Show More Authors

Background: One of the unique prosthesis for tooth or teeth replacement is the dental implant. Our attempt is using a biomaterial system that is easily obtained and applicable and has the ability to provoke osteoinductive growth factor to enhance bone formation at the site of application. One of these natural polymers is hyaluronic acid. Material and methods: Sixty machined surface implants from commercially pure titanium rod inserted in thirty NewZealand rabbits. Two implants placed in both tibia of each rabbit. The animals scarified at 1, 2 and 4 weeks after implantation (10 rabbits for each interval). For all of animals the right tibia’s implant was control (uncoated) and the left one was experimental (coated with 0.1ml Hyaluro

... Show More
View Publication Preview PDF
Crossref (6)
Crossref
Publication Date
Wed Dec 14 2022
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesis, characterization, theoretical study and biological evaluation of Schiff base and their La(III), Ce(IV) and UO2(II) complexes
...Show More Authors

ABSTRACT. A new three metal complexes of La(III), Ce(IV) and UO2(II) ions have been synthesized based on a Schiff base derived from the condensation of L-histidine and anisaldehyde. All prepared compounds were characterized by different spectroscopic techniques and Density-functional theory (DFT) calculations. The complexes were proposed to have an octahedral structure based on the investigated results. The optimized shape, numbering system, and dipole moment vector of Ligand and La, Ce, and UO2 (1:1) chelates were investigated. The Schiff base ligand and complexes exhibit moderate action against all of the bacteria tested, with P. aeruginosa, Klebsiella sp., and E. faecalis respectively being the order of inhibition.  

... Show More
View Publication
Crossref (6)
Crossref