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
Wed Oct 18 2023
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Nurses’ Practices Concerning Isolation Techniques for Adult Leukemic Patients in Baghdad Teaching Hospitals
...Show More Authors

Objective: To evaluate nurses' practices concerning isolation techniques for Adult Leukemic Patients (ALP).
Methodology: A descriptive study was carried out at the isolation rooms at leukemic wards in Baghdad Teaching
Hospitals, starting from Jan. 27th 2008 up to the 27th of Apr. 2008. To achieve the objectives of study, a non-probability
"purposive" sample of (50) nurse was selected out of four Teaching Hospitals in Baghdad city were selected according
to the criteria of the study sample.
The study instrument consisted of two major parts. It is based on the review of literature. First is concerned with
demographic data for nurses; and the second part is observational tool (checklist) is composed of (83) item. The conte

... Show More
View Publication Preview PDF
Publication Date
Wed Mar 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Cold Cracking Technology for Crude Oil Upgrading in Qaiyarah Heavy Oil Field; Technical and Economical Evaluation
...Show More Authors

Heavy oil is classified as unconventional oil resource because of its difficulty to recover in its natural state, difficulties in transport and difficulties in marketing it. Upgrading solution to the heavy oil has positive impact technically and economically specially when it will be a competitive with conventional oils from the marketing prospective. Developing Qaiyarah heavy oil field was neglected in the last five decades, the main reason was due to the low quality of the crude oil resulted in the high viscosity and density of the crude oil in the field which was and still a major challenge putting them on the major stream line of production in Iraq. The low quality of the crude properties led to lower oil prices in the global markets

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sat Dec 15 2018
Journal Name
Journal Of Baghdad College Of Dentistry
Immunohistochemical expression of endocan, as a marker of assessment of angiogenic potential in benign vascular lesions (hemangioma, lymphangioma and lobular capillary hemangioma) of head and neck region
...Show More Authors

 BACKGROUND: Vascular tumors are a heterogeneous group of diseases with biological behavior ranging from a hamartomatous growth to frank malignant. The pathophysiology of lymphangioma, vascular malformation and hemangioma is interconnected, blood vessels known to be the site of origin of hamartomas, venous malformations and some neoplasms as benign, tumor-like growth of vessels (hemangiomas). Angiogenesis is the process of formation of new blood vessels from an existing structure.

Aims of study Assessment of angiogenic potential in benign vascular lesions (hemangioma, lymphangioma and lobular capillary hemangioma) of head and neck region.

 Materials and Methods: Twenty-two formalin-fixed paraffin-embedd

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

Scopus (10)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Fri Nov 03 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synergistic Effects of 2-Deoxy-D-Glucose and Cinnamic Acid with Erlotinib on NSCLC Cell Line
...Show More Authors

Background: In spite of all efforts, Non-small cell lung cancer (NSCLC) is a fatal solid tumor with a poor prognosis as of its high metastasis and resistance to present treatments. Tyrosine kinase inhibitors (TKI) such as erlotinib are efficient in treating NSCLC but the emergence of chemoresistance and adverse effects substantially limits their single use. Objective: in this study, the combination treatments of either 2-deoxy-D-glucose (2DG) or cinnamic acid (CINN) with erlotinib (ERL) were tested for their possible synergistic effect on the proliferation and migration capacity of NSCLC cells. Methods: In this study, NSCLC model cell line A549 was used to investigate the effects of single compounds and their combination on cell gro

... Show More
View Publication
Scopus (5)
Crossref (3)
Scopus Crossref
Publication Date
Mon Mar 13 2023
Journal Name
Diagnostics
The Effect of a Bioactive Oral System and CO2 Laser on Enamel Susceptibility to Acid Challenge
...Show More Authors

This study evaluated the structural changes of enamel treated by the Regenerate system and carbon dioxide (CO2) laser against acid challenge. Thirty human enamel slabs were prepared and assigned into three groups: Group I: untreated (control); Group II: treated with the Regenerate system; and Group III exposed to CO2 laser. All specimens were subjected to an acid challenge (pH 4.5–7.0) for 14 days. Specimens were evaluated and compared at 120 points using five Raman microspectroscopic peaks; the phosphate vibrations ν1, ν2, ν3, and ν4 at 960, 433, 1029, and 579 cm−1, respectively, and the carbonate at 1070 cm−1, followed by Vickers microhardness test. The ratio of carbonate to phosphate was correlated to the equivalent mic

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (6)
Scopus Clarivate Crossref
Publication Date
Wed Feb 14 2024
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

View Publication
Scopus (10)
Crossref (10)
Scopus Crossref
Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of General Chemistry
Preparation, Characterization, and Biological Activity of Mixed Schiff Base Ligand Complexes with Amino Acid L-Proline
...Show More Authors

View Publication
Scopus (10)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Sun Jan 01 2023
Journal Name
Chemical Methodologies
Cytotoxicity and Anticancer Effect of Chitosan-Ag NPs-Doxorubicin-Folic Acid Conjugate on Lungs Cell Line
...Show More Authors

This study looked at how the synthetic chitosan-AgNPs-Doxorubicin-folic acid combination affected the A549 cell line in terms of cytotoxicity and anticancer activity. By reducing silver nitrate (AgNO3) and biodegradable chitosan, silver nanoparticles were biosynthesized. The produced conjugate was examined by using FT-IR spectroscopy, atomic force microscopy (AFM), and field emission scanning electron microscopy (FE-SEM). The cytotoxicity assay for the viability of A549 cells revealed that the combination of chitosan, AgNPs, doxorubicin, and folic acid decrease cell viability in a dose-determined by method over 48 hours, which direct to a dependent reduce in the activity of A549 cells. The mechanism analysis of the impacted living cells lea

... Show More
View Publication Preview PDF
Scopus (30)
Scopus
Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Comparative Evaluation of Using Intranasal Desmopressin, Parenteral Diclofenac or their Combination in the Management of Acute Renal Colic Pain in Iraqi Patients
...Show More Authors

         There is a suggestion that an antidiuretic hormone-induced decrease in diuresis might contribute to the rapid relief of the acute pain in renal colic. This study was designed to evaluate the efficacy of desmopressin nasal spray compared with diclofenac given intramuscularly in patients with acute renal colic. The study included 75 patients randomized into three different groups; group A received desmopressin (40 μg, nasal spray), group B diclofenac (75 mg) intramuscularly and group C, both desmopressin and diclofenac. Pain was assessed using a visual analogue scale (a 10-cm horizontal scale ranging from `no pain' to `unbearable pain') at baseline, 10, 20 and 30 min after administering t

... Show More
View Publication Preview PDF
Crossref (1)
Crossref