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
Thu May 12 2016
Journal Name
Biochemistry
Probing the Role of Active Site Water in the Sesquiterpene Cyclization Reaction Catalyzed by Aristolochene Synthase
...Show More Authors

View Publication
Crossref (24)
Crossref
Publication Date
Sun May 05 2024
Journal Name
Technium Business And Management
Measuring Blue Ocean Leadership activities in public organizations: field research in the Ministry of Communications
...Show More Authors

This study aims to identify the level of application of blue ocean leadership activities in public organizations and to build a conceptual and cognitive framework around this concept. The study adopted a descriptive-analytical approach, and the research sample consisted of (95) individuals from the senior management working at the center of the Iraqi Ministry of Communications (director general, department manager, section head). The data analysis technique used is structural equation modeling (SEM) and the Statistical Package for the Social Sciences (SPSS). The results indicate that the senior management in the Ministry of Communications is working to adopt the blue ocean leadership style through its activities, but not to the leve

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Dec 30 2019
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis and Characterization of Nano Y Zeolite Using MWCNT as Media for Crystal Growth
...Show More Authors

   The present research was conducted to synthesis Y-Zeolite by sol-gel technique using MWCNT (multiwalled carbon nanotubes) as crystallization medium to get a narrow range of particle size distribution with small average size compared with ordinary methods. The phase pattern, chemical structure, particle size, and surface area were detected by XRD, FTIR, BET and AFM, respectively. Results shown that the average size of Zeolite with and without using MWCNT were (92.39) nm and (55.17) nm respectively .Particle size range reduced from (150-55) nm to (130-30) nm. The surface area enhanced to be (558) m2/g with slightly large pore volume (0.231) km3/g was obtained. Meanwhile, degree of crystallization decrease

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon May 01 2017
Journal Name
Journal Of Stored Products Research
Detection and prediction of Sitophilus oryzae infestations in triticale via visible and near-infrared spectral signatures
...Show More Authors

Triticale is a hybrid of wheat and rye grown for use as animal feed. In Florida, due to its soft coat, triticale is highly vulnerable to Sitophilus oryzae L. (rice weevil) and there is interest in development of methods to detect early-instar larvae so that infestations can be targeted before they become economically damaging. The objective of this study was to develop prediction models of the infestation degree for triticale seed infested with rice weevils of different growth stages. Spectral signatures were tested as a method to detect rice weevils in triticale seed. Groups of seeds at 11 different levels (degrees) of infestation, 0–62%, were obtained by combining different ratios of infested and uninfested seeds. A spectrophotometer wa

... Show More
View Publication
Scopus (7)
Crossref (6)
Scopus Clarivate Crossref
Publication Date
Mon Mar 30 2009
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Prediction of bubble size in Bubble columns using Artificial Neural Network
...Show More Authors

In the literature, several correlations have been proposed for bubble size prediction in bubble columns. However these correlations fail to predict bubble diameter over a wide range of conditions. Based on a data bank of around 230 measurements collected from the open literature, a correlation for bubble sizes in the homogenous region in bubble columns was derived using Artificial Neural Network (ANN) modeling. The bubble diameter was found to be a function of six parameters: gas velocity, column diameter, diameter of orifice, liquid density, liquid viscosity and liquid surface tension. Statistical analysis showed that the proposed correlation has an Average Absolute Relative Error (AARE) of 7.3 % and correlation coefficient of 92.2%. A

... Show More
View Publication Preview PDF
Publication Date
Sat Dec 30 2023
Journal Name
Iraqi Journal Of Science
Application of 2D Electrical Resistivity Method and Ground Penetration Rader for Detection of the Archaeological Remains in Kish Site, Babylon, Iraq
...Show More Authors

     The 2D electrical resistivity imaging (ERI) is a non-destructive method with good efficiency to detect shallow subsurface features. The archeological subsurface features were investigated with this method in most cases with the assistance of other methods such as GPR method. Eleven 2D ERI profiles were carried out to investigate the subsurface archeological features in the Kish site in the Babylon area. The 2D electrical resistivity survey was achieved with ABEM Terrameter-LS2 Device and 30 electrodes with 1-meter spacing between the adjacent electrodes along each profile. The length of the profile is 29 meters and the spacing between the adjacent profiles is 3 meters. The software RES2DINV was used to obtain the final inverted

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Mon Mar 15 2021
Journal Name
Al-adab Journal
Alienation in Scapegoat novel by Elie Amir
...Show More Authors

 تهدف هذه الدراسة إلى بحث ظاهرة الاغتراب في رواية " ديك الفداء " لايلي عامير ، لأن هذه الظاهرة تبدو أكثر وضوحا في هذه الرواية ، وتمثل تیارا مسيطرة على معطياتها واتجاهاتها الفكرية والفنية، خاصة أن الكاتب استطاع أن يجسد هذه الظاهرة المحورية تجسيدا فنيا متميزا ، وكشف عن طبيعة العلاقة بين عالم الواقع وعالم الحلم لدى الشخصيات، وعما تتسم به من تناقض و تعارض وتصادم و شعور بالإحباط والضياع والاغتراب. وقد اشتملت ال

... Show More
View Publication Preview PDF
Publication Date
Fri May 01 2020
Journal Name
Journal Of Engineering
Semi-Analytical Prediction of Flank Tool Wear in Orthogonal Cutting of Aluminum
...Show More Authors

This study aims to model the flank wear prediction equation in metal cutting, depending on the workpiece material properties and almost cutting conditions. A new method of energy transferred solution between the cutting tool and workpiece was introduced through the flow stress of chip formation by using the Johnson-Cook model. To investigate this model, an orthogonal cutting test coupled with finite element analysis was carried out to solve this model and finding a wear coefficient of cutting 6061-T6 aluminum and the given carbide tool.

View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Dec 01 2013
Journal Name
Political Sciences Journal
Activities of International Studies Branch
...Show More Authors

نشاطات فرع الدراسات الدولية

View Publication Preview PDF
Crossref
Publication Date
Thu Apr 11 2019
Journal Name
Political Sciences Journal
Scientific Activities College of branches
...Show More Authors

Scientific Activities College of branches

View Publication Preview PDF
Crossref