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
Fri Jan 31 2025
Journal Name
Journal Of Baghdad College Of Dentistry
An evaluation of three fissure sealants microleakage with presence or absence of bonding agent through time intervals (In vitro study)
...Show More Authors

Background: Pit and fissure sealant have been considered an outstanding adjunct to oral health care in the decrease of occlusal caries onset and low progression. The aims of this in vitro study were to evaluate the marginal microleakage of three different types of fissure sealants (SDI, Tg and tetric N-flow) by time interval, one day and 45 days, in the presence or absence of bonding agent among maxillary and mandibular teeth. Materials and methods: Seventy two sound human maxillary and mandibular first premolar teeth were collected which were free from obvious carious lesions. The teeth were randomly divided into two main equal groups, group (1) and group (2), each group consists of (36) teeth involving equal numbers of maxillary and mandi

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Detection of Anti-Helicopacter pylori IgG Antibody, Anti-GAD antibody, Anti-Beta islets cell in a sample of serum with type-2 Diabetes mellitus patients
...Show More Authors

We have investigated twenty five patients with type-2 diabetes mellitus aged (35-60) years and fifteen healthy persons as control group to detect Anti-Helicobacter pylori IgG antibody. All studied groups were carried out to measure fasting blood sugar, anti- Glutamic acid decarboxylase (GAD), anti-? islets cells antibody by IFAT, Anti-H. pylori IgG antibody by ELISA technique. There was significant elevation in the concentration of fasting blood sugar than in control group (P < 0.05), the patients had negative results for anti-GAD antibody and anti- ? islets cells antibody, there were significant differences (P < 0.05) of anti-H. pylori IgG antibody in 28 % of patients had type-2 diabetes than control group. This lead to suggestion that typ

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Jun 15 2019
Journal Name
Journal Of Baghdad College Of Dentistry
Perineural Invasion in Oral Squamous Cell Carcinoma in Relation to Tumor Depth
...Show More Authors

Background: The American Joint committee on Cancer in their 8th edition staging manual regarded perineural invasion as one of the most important prognostic factors for Lip and Oral Cavity Squamous Cell Carcinoma, it also incorporated tumor depth of invasion in defining tumor size category in the new staging system. This study was conducted to evaluate the frequency of perineural invasion in oral squamous cell carcinoma and the effect of approaching tumor depth in this process. Materials and Methods: fifty-four formalin fixed paraffin embedded tissue blocks of radical resections of Oral Squamous Cell Carcinoma were cut and stained with Hematoxylin and Eosin stain, then evaluated for perineural invasion, with estimation of tumor depth of i

... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Wed Aug 19 2020
Journal Name
Revista De Chimie
Synthesis, Characterization and Biological Evaluation of Cr(III), Fe(III), Co(II), Ni(II), Zn(II) and Cd(II) Complexes Using an Azo Dye as Ligand
...Show More Authors

Azo ligand 11-(4-methoxyphenyl azo)-6-oxo-5,6-dihydro-benzo[4,5] imidazo[1,2-c] quinazoline-9-carboixylic acid was derived from 4-methoxyaniline and 6-oxo-5,6-dihydro-benzo[4,5]imidazo[1,2-c]quinazoline-9-carboxylic acid. The presence of azo dye was identified by elemental analysis and spectroscopic methods (FT-IR and UV-Vis). The compounds formed have been identified by using atomic absorption in flame, FT.IR, UV-Vis spectrometry magnetic susceptibility and conductivity. In order to evaluate the antibacterial efficiency of ligand and its complexes used in this study three species of bacteria were also examined. Ligand and its complexes showed good bacterial efficiencies. From the obtained data, an octahedral geometry was proposed for all p

... Show More
Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Clinical Evaluation of Orphenadrine citrate as a Plain Tablet
...Show More Authors

Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .

      Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .

    The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Nystatin Microparticles as a Sustained Release System
...Show More Authors

Nystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Sat Oct 30 2021
Journal Name
Iraqi Journal Of Science
The Stress-Inducible Heat Shock Protein 70 (HSPA1A) as A Novel Biomarker in Lung Tumors: A Promoting Study
...Show More Authors

     Heat shock proteins (HSPs) are a group of intracellular proteins that promote proteins folding and unfolding under normal and/or stress conditions. In addition to their intracellular location, HSPs are found on the plasma membranes of stressed, but not normal, cells and in the extracellular milieu where they can trigger an immune response. For instance, the inducible form of heat shock protein 70 (HSPA1A) was found to be overexpressed, intra or extracellularly, by many types of stressed cells. In our study, we aim to investigate the levels of HSPA1A in the serum of untreated lung tumor patients and its expression in the tissues derived from lung tumors and chronic obstructive pulmonary diseases (COPD) and healthy

... Show More
View Publication Preview PDF
Scopus (1)
Scopus Crossref
Publication Date
Tue Jul 09 2019
Journal Name
Journal Of Global Pharma Technology
Ni (II) and Cd (II) Complexes Derivatives from Heterocyclic Schiff Base; Synthesis, Spectroscopic and Biological Studies
...Show More Authors

Ni and Cd complexes of new Schiff base derived from 5-Amino-2-phenyl-2,4-dihydro-pyrazol-3-one with 4-chlorobenzalaldehyde (A) , 2-Hydroxy-benzalaldehyde (B) and 4-Hydroxy-benzaldehyde (C) have been prepared and characterized by elemental analysis , molar conductivity measurements , FTIR , UV- vis , 1HNMR, mass spectrometer and magnetic susceptibility. Analytical data revealed that six complexes were a distorted tetrahedral geometry and exhibited (1:1) metal :ligand ratio. The biological activity for the three ligands and its complexes were studied

Publication Date
Thu Jun 01 2023
Journal Name
Russian Journal Of Organic Chemistry
New Quinolin-2-one, Indazole, and Benzisoxazole Derivatives Derived from Chalcones: Synthesis, Characterization, and Biological Activity
...Show More Authors

View Publication
Scopus (4)
Crossref (3)
Scopus Clarivate Crossref
Publication Date
Fri Jun 29 2018
Journal Name
Journal Of The College Of Education For Women
Stream of Consciousness Technique: Psychological Perspectives and Use in Modern Novel
...Show More Authors

Stream of Consciousness technique has a great impact on writing literary texts in the modern age. This technique was broadly used in the late of nineteen century as a result of thedecay of plot, especially in novel writing. Novelists began to use stream of consciousness technique as a new phenomenon, because it goes deeper into the human mind and soul through involving it in writing. Modern novel has changed after Victorian age from the traditional novel that considers themes of religion, culture, social matters, etc.  to be a group of irregular events and thoughts interrogate or reveal the inner feeling of  readers.

This study simplifies stream of consciousness technique through clarifying the three levels of conscious

... Show More
View Publication Preview PDF