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
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Effect of Silver Oxide Film Thickness on Some Optical Parameter
...Show More Authors

Films of silver oxide of different thickness have been prepared by the chemical spray paralysis. Transmission and absorption spectra have recorded in order to study the effect of increasing thickness on some optical parameter such as reflectance, refractive index , and dielectric constant in its two parts . This study reveals that all these paramters affect by increasing the thickness .

View Publication Preview PDF
Crossref
Publication Date
Thu Dec 31 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Measuring the Impact of Commitment to Apply Banking Governance Mechanisms
...Show More Authors

This research aims to measure the impact of applying bank governance mechanisms in reducing the financial risks of banks listed on the Palestine Stock Exchange, and to answer research questions and test hypotheses for the study, researchers adopted the descriptive and analytical approach, and data were collected from the annual financial reports of the banks listed on the Palestine Exchange during the period between (2009-2018), as a time series for the purpose of finding, analyzing and measuring the effect between the study variables during this period by (60) views for each of the study variables, using the statistical analysis program views(9) to enter, process and analyze the data. The results of the study proved that there i

... Show More
View Publication Preview PDF
Publication Date
Sun May 22 2005
Journal Name
University Of Technology
Results Of The Factor Group CF(G,Z)/R(G)
...Show More Authors

Publication Date
Fri Jun 12 2026
Journal Name
Journal Of Engineering
Application of Mathematical Drilling Model on Southern Iraqi Oil Fields
...Show More Authors

View Publication
Publication Date
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Improved Automatic Registration Adjustment of Multi-source Remote Sensing Datasets
...Show More Authors

Registration techniques are still considered challenging tasks to remote sensing users, especially after enormous increase in the volume of remotely sensed data being acquired by an ever-growing number of earth observation sensors. This surge in use mandates the development of accurate and robust registration procedures that can handle these data with varying geometric and radiometric properties. This paper aims to develop the traditional registration scenarios to reduce discrepancies between registered datasets in two dimensions (2D) space for remote sensing images. This is achieved by designing a computer program written in Visual Basic language following two main stages: The first stage is a traditional registration process by de

... Show More
Crossref (1)
Crossref
Publication Date
Thu Mar 01 2007
Journal Name
Journal Of Engineering
DEWAXING OF DISTILLATE OIL FRACTION (400- 500 ºC) USING UREA
...Show More Authors

De-waxing of lubricating oil distillate (400-500 ºC) by using urea was investigated in the present study. Lubricating oil distillate produced by vacuum distillation and refined by furfural extraction was taken from Al-Daura refinery. This oil distillate has a pour point of 34 ºC. Two solvents were used to dilute the oil distillate, these are methyl isobutyl ketone and methylene chloride. The operating conditions of the urea adduct formation with n-paraffins in the presence of methyl isobutyl ketone were studied in details, these are solvent to oil volume ratio within the range of 0 to 2, mixer speed 0 to 2000 rpm, urea to wax weight ratio 0 to 6.3, time of adduction 0 to 71 min and temperature 30-70 ºC). Pour point of de-waxed oil and yi

... Show More
View Publication Preview PDF
Publication Date
Tue Nov 17 2015
Journal Name
International Journal Of Computer Applications
Categorization of ‘Holy Quran-Tafseer’ using K-Nearest Neighbor Algorithm
...Show More Authors

View Publication
Crossref (1)
Crossref
Publication Date
Wed Oct 01 2008
Journal Name
Journal
Topical therapy of xeroderma pigmentosa with 20% zinc sulfate solution
...Show More Authors

S Khalifa E, N Adil A, K Nabeel O…, 2008

View Publication
Publication Date
Fri Jun 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Revitalization of a necrotic immature permanent anterior tooth (Case Report)
...Show More Authors

Background: Management of immature permanent teeth with necrotic pulp is considered challenging to the clinician. Regeneration of pulp tissue is a relatively new approach for management of these teeth that allow continuation of root maturation rather than formation of just a calcific barrier as in apexification. Method: 9 years-old girl with traumatized upper left central incisor. The clinical and radiographical examinations revealed uncomplicated crown fracture, tenderness to percussion, absence of response to cold vitality test. Diagnostic X-ray revealed open apex with periapical radiolucency. Revascularization was suggested to treat the tooth, starting with irrigation of canal with 5% NaOCl + 3% H2O2, followed by 2 weeks of triple antibi

... Show More
View Publication
Crossref
Publication Date
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Deterministic Analysis of Wind Loads Effects on High-Rise Buildings
...Show More Authors

This paper studies the effect of mean wind velocity on tall building. Wind velocity, wind profile and wind pressure have been considered as a deterministic phenomenon. Wind velocity has been modelled as a half-sinusoidal wave. Three exposures have been studied B, C, and D. Wind pressure was evaluated by equation that joined wind pressure with mean wind velocity, air density, and drag coefficient.

Variations of dynamic load factor for building tip displacement and building base shear were studied for different building heights, different mode shapes, different terrain exposures, and different aspect ratios of building plan. SAP software, has been used in modelling and dynamic analysis for all case studies.

... Show More
View Publication Preview PDF