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 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Derivatives Tetrazoles for Trimethoprim Drug
...Show More Authors

The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.

View Publication Preview PDF
Crossref
Publication Date
Tue Feb 10 2015
Journal Name
Al-qadisiyah Journal For Science
*Synthesis, spectral studies and antimicrobial evaluation of 6,6--(1,2-benzenediazo) bis (3-amino benzoic acid) complexes with some metal ions
...Show More Authors

The Ligand 6,6--(1,2-benzenediazo) bis (3-aminobenzoicacid) derived from o-phenylenediamine and 3-aminobenzoicacid was synthesized. The prepared ligand was identified by Microelemental Analysis, 1HNMR, FT-IR and UV-Vis spectroscopic techniques. Treatment of the ligand with the following metal ions (CoII, NiII, CuII and ZnII ) in aqueous ethanol with a 1:1 M:L ratio and at optimum pH. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR and UV-Vis, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). H

... Show More
Publication Date
Sat Jun 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis and Evaluating the Antimicrobial Activities of Various Adducts Prepared from Isatins and Proline
...Show More Authors

characteristic tissues and cells, exerting their pharmacological aspects and alleviating a lot of diseased processes. Accordingly, this research is about introducing some isatins to be nucleophilically attacked at C3 forming products of azomethine ylide functionality. These iminium compounds were made by allowing certain isatins to be reacted with the secondary amino acid, proline, at acetic acid and methanol medium and then collected after purification to be identified with total Leukocyte count (TLC) and melting point. The structural characterization was performed by fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), and community health nursing (CHN) analysis. The microbiological evaluatio

... Show More
View Publication
Scopus Crossref
Publication Date
Sun Jul 02 2023
Journal Name
Iraqi Journal Of Science
Evaluation of Anti-Helicobacter pylori Antibodies in A group of Iraqi Patients with Atherosclerosis and Coronary Artery Disease
...Show More Authors

Evaluation of Anti-Helicobacter pylori Antibodies in A group of Iraqi Patients with Atherosclerosis and Coronary Artery Disease

View Publication Preview PDF
Publication Date
Sun Jul 02 2023
Journal Name
Iraqi Journal Of Science
Evaluation of Anti-Helicobacter pylori Antibodies in A group of Iraqi Patients with Atherosclerosis and Coronary Artery Disease
...Show More Authors

Evaluation of Anti-Helicobacter pylori Antibodies in A group of Iraqi Patients with Atherosclerosis and Coronary Artery Disease

View Publication
Publication Date
Thu Jun 29 2023
Journal Name
Farmacia
CORRELATION BETWEEN INTEGRIN ALPHA-4 GENE POLYMORPHISMS AND FAILURE TO RESPOND TO NATALIZUMAB THERAPY IN IRAQI MULTIPLE SCLEROSIS PATIENTS
...Show More Authors

View Publication
Scopus (1)
Scopus Clarivate Crossref
Publication Date
Mon Sep 30 2024
Journal Name
South Eastern European Journal Of Public Health
Antimicrobial Efficacy of a Novel Herbal Endodontic Irrigant Against Enterococcus Faecalis in Root Canals of Permanent Teeth: An in Vitro Study
...Show More Authors

Background: A successful endodontic treatment is aimed at the sterilization of the entire pulp space. The use of extracts from Rhamnus prinoides as a novel irrigating material for root canal has not been studied . Hence, the antimicrobial efficacy of the alcoholic extract of Rhamnus prinoides as an irrigation material against E. faecalis was evaluated in comparison with the 2.5% sodium hypochlorite (NaOCL) solution used for root canals of permanent teeth. Methods: A total of 30 single-rooted human permanent teeth were thoroughly cleaned, shaped, and disinfected. Then, each tooth was subjected to a two-week infection with Enterococcus faecalis at 37 °C . Afterward, the samples were divided into three groups (10 teeth per group): 0.9

... Show More
View Publication
Crossref
Publication Date
Mon Feb 13 2023
Journal Name
Journal Of Educational And Psychological Researches
Evaluation of Activities and Evaluation Questions Implied in the Content of the Computer Textbook for the Fifth Preparatory Grade According to Creative Thinking and Developing Suggestions
...Show More Authors

The current research aims to evaluate the activities and evaluation questions implied in the content of the computer textbook for the fifth preparatory grade according to the creative thinking and developing suggestions through answering the following question: what is the percentage of creative thinking skills in the content of the computer textbook for the fifth Preparatory grade students issued by the Iraqi Ministry of Education/ Directorate General of the curriculum in the academic year (2019-2020)? The researchers followed the descriptive-analytical approach.  The research community was determined by the content of the computer textbook for the fifth preparatory grade. As for the research sample, it was limited to all activitie

... Show More
View Publication Preview PDF
Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives
...Show More Authors

 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as

... Show More
View Publication Preview PDF
Scopus (4)
Crossref (2)
Scopus Crossref
Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and characterization of some new thiazolidinone derivatives containing indole ring
...Show More Authors

Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII] a, b and [VIII] a, b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII] a, b,[VIII] a, b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX] a, b and [X] ad). Finally, the new derivatives [XI] ac run out via the reacted compound [IX] a with different n-alkyl bromide (methyl bromide, ethyl bromide, and butyl bromide)