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 Sep 04 2016
Journal Name
Baghdad Science Journal
Synthesizing, Characterizing and Studying the Biological Activity of Some New Schiff-Bases Derivatives Containing the Monosaccharide Moiety
...Show More Authors

A new series of ?-D-glucose as Schiff bases derivatives is synthesized and characterized with studying their bioactivity. Hydroxyl groups at C (1,2&5,6) sugar moiety are converted into acetal form through a reaction with dry acetone using phosphoric acid and anhydrous zinc chloride as catalysts producing 1,2:5,6-di-O-isopropyledine ?-D-glucofuranose(I). The five memberd ring acetal of C(5,6) is hydrolyzed with acetic acid (65%)and a reaction of the new product with sodium periodate is carried on to get an aldehyde moiety which is used to produce a new series of Schiff bases through reacting with different amino compounds such as 4-amino antipyrene . The suggested chemical structures of the prepared compounds are confirmed by using UV., FT

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Dec 01 2010
Journal Name
Al Mustansiriyah Journal Of Pharmaceutical Sciences
Evaluation ofAaspirin, Clopidogrel or Their Combination In Hypertensive Patients
...Show More Authors

The objective of this study is to evaluate the effect of aspirin, clopidogrel or their combination on different parameters in hypertensive patients.Platelets adhesion, activation, and aggregation are central to thrombus formation, which follows atherosclerotic plaque disruption and causes acute coronary syndromes. Aspirin and clopidogrel exert their antiplatelet effects by inhibiting thromboxane A2 production and adenosine diphosphate–induced platelet aggregation pathways, respectively. This study was designed to evaluate the possible effects of aspirin and clopidogrel given either alone or in combination in patients with essential hypertension on blood pressure and other parameters in addition to lipid profile using a randomized

... Show More
Crossref
Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Advanced Pharmacy Education And Research
Formulation and evaluation of mucoadhesive buccal tablet of Anastrozole
...Show More Authors

View Publication Preview PDF
Scopus (8)
Crossref (6)
Scopus Crossref
Publication Date
Tue Feb 01 2022
Journal Name
Baghdad Science Journal
New Tetra-dentate Schiff Base Ligand N2O2 and Its Complexes with Some of Metal Ions: Preparation, Identification, and Studying Their Enzymatic and Biological Activities
...Show More Authors

In present work, new tetra-dentate ligand, titled 3,5-bis ((E)-5-Bromo-2-hydroxy benzylidene amino) benzoic acid (H3L), was prepared via an acid-catalyzed condensation process. New four metallic ligand complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions, were also prepared from the refluxing of equivalent moles. Ligand's structure and its complexes; were confirmed by numerous characterization methods, including Ultraviolet-Visible, Infrared, Mass Spectrometer, 1H and 13C Nuclear Magnetic Resonance spectra, atomic absorption, magnetic moments, and molar conductivity measurements. The results of the spectroscopic analyzes proved that the prepared ligand acts as tetradentate bi-ionic ligand and it was bond

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Wed May 08 2024
Journal Name
Babylon: Abjad Publising House
“Translation is the Art of Negotiating with Words”, in Hassad aS-Sineen(Harvest of Years): Essays in Teaching Translation
...Show More Authors

Publication Date
Wed May 31 2023
Journal Name
Iraqi Geological Journal
Studying the Effect of Permeability Prediction on Reservoir History Matching by Using Artificial Intelligence and Flow Zone Indicator Methods
...Show More Authors

The map of permeability distribution in the reservoirs is considered one of the most essential steps of the geologic model building due to its governing the fluid flow through the reservoir which makes it the most influential parameter on the history matching than other parameters. For that, it is the most petrophysical properties that are tuned during the history matching. Unfortunately, the prediction of the relationship between static petrophysics (porosity) and dynamic petrophysics (permeability) from conventional wells logs has a sophisticated problem to solve by conventional statistical methods for heterogeneous formations. For that, this paper examines the ability and performance of the artificial intelligence method in perme

... Show More
View Publication
Scopus (5)
Crossref (2)
Scopus Crossref
Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Evaluation the Emotional Intelligence of Administrative and Audit leaderships in the Federal Board of Supreme Audit to achieve audit Effectiveness
...Show More Authors

The Psychologists have noticed, not long ago, that the man’s success and happiness in life do not only depend on his degree and education, which express on his mental intelligence but also they need another kind of intelligence called emotional intelligence. The research aims at identifying the emotional intelligence level of the top and administrative leaderships in the Federal Board of Supreme Audit by evaluating their emotional intelligence when the administrative and audit leaderships face emotional interactions by dealing with administrative and audit stuffs in the Board. The research problem is focused on the following question “Is the emotional intelligence of the top and administrative leaderships in the Fede

... Show More
View Publication Preview PDF
Publication Date
Wed Dec 15 2010
Journal Name
Iraqi Journal Of Laser
Evaluation the Effect of 805 nm Wavelength Diode Laser on Repair of Mandibular Bone Repair and Skin Incisions in Rabbits
...Show More Authors

The long healing time of bone after tooth extraction in order to construct artificial teeth is uncomfortable to the patient because of aesthetic or masticatory problems in addition to the daily visit to dental clinic. The objective of this study was to evaluate the effect of 805 nm diode laser with long time intervals on repair of bone and skin incisions in rabbits through biochemical, radiological and histological findings. Eighteen New-Zealand rabbits were undergone surgical operations to make a cavity in the bone of the lower jaw, the rabbits were divided into two groups:- Group A (control group) containing nine rabbits. Group B (lased group) containing nine rabbits in which two cavities were done, one on the right side and the other

... Show More
View Publication Preview PDF
Publication Date
Thu Feb 29 2024
Journal Name
International Journal Of Design & Nature And Ecodynamics
Artificial Neural Network Assessment of Groundwater Quality for Agricultural Use in Babylon City: An Evaluation of Salinity and Ionic Composition
...Show More Authors

View Publication Preview PDF
Scopus (4)
Crossref (3)
Scopus Crossref
Publication Date
Fri Mar 01 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Evaluation of accounting procedures for joint arrangements in the Iraqi environment and their reflection on the quality of financial reporting
...Show More Authors

The research aims to assess the local accounting procedures related in one of developments that have taken place, and largely on the structure of the Iraqi economic activity. But a partnership between the (public and private sector), or one of the types of joint arrangements, and through the use of the analytical method and extrapolate the reality of the accounting treatments in Company research sample. Research found to a number of conclusions that the unified accounting system applied in the economic units that deal with contracting joint arrangements formula suffers from obvious shortcomings, and reflected the common arrangements suffer from obvious shortcomings. and reflected on the quality of financial reporting, and the urgent need

... Show More
View Publication Preview PDF
Crossref