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
Tue Dec 22 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Continuous improvement of technology and its role In reducing the costs in accordance with the management style On the basis of the activities (ABM): Applied Research in the General Company for Textile Industries / hula
...Show More Authors

The administration on the basis of the activities designed to evaluate the performance of activities in terms of cost, time and quality by identifying activities that add value and those that are no add value and  enables the administration of making up their own continuous improvement in production, through lower costs and reduce the time and improve the quality   and reduce the incidence of spoilage and waste, y based search Ally premise that (the continuous improvement of the adoption of management style on the basis of the activities helps management in decision-making wise to reduce  costs) to prove the hypothesis has sought research to achieve its goal of  Alkadivh and Alkoppelan     &nb

... Show More
View Publication Preview PDF
Publication Date
Thu Feb 06 2025
Journal Name
Journal Of Baghdad College Of Dentistry
A Clinical Method for Prediction of Alveolar Bone Mineral Density in the Area between the Second Premolar and First Molar in Iraqi Adults with Class I Occlusion
...Show More Authors

Background: Orthodontic mini-implants are increasingly used in orthodontics and the bone density is a very important factor in stabilization and success of mini-implant. The aim of this study was to observe the relationship among maximum bite force (MBF); body mass index (BMI); face width, height and type; and bone density in an attempt to predict bone density from these variables to eliminate the need for CT scan which have a highly hazard on patient. Materials and Methods: Computed tomographic (CT) images were obtained for 70 patients (24 males and 46 females) with age range 18-30 years. The maxillary and mandibular buccal cortical and cancellous bone densities were measured between 2nd premolar and 1st molar at two levels from the alveol

... Show More
View Publication Preview PDF
Publication Date
Sun Mar 02 2008
Journal Name
Baghdad Science Journal
Effect of Volatile Oil of Myrtus communis on growth and activities of some types of Pathogenic Bacteria and Candida albicans
...Show More Authors

This Study aimed to studying the effect of Volatile oil extracted from the leaves of Myrtus communis on the growth and activities of the following types of bacteria: Staphylococcus aureus, Streptococcus pyogenes, Klebsilla pneumoniae, Pseudomonas aeruginosa, and the yeast Candida albicans. The results showed an inhibitory effect of the oil on both the growth and activity of the tested microbes. This was reflected by the minimum inhibitory concentration (MIC) of Staphylococcus aureus, Streptococcus pyogenes, Klebsilla pneumoniae, Pseudomonas aeruginosa which was: (2.5, 1.25, and 2.5,5 % respectively), and the yeast (5) %. Also, the Minimum bactericidal concentration (MBC) to the bacteria mentioned above was (5, 2.5,5,10 % respectivel

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Oct 26 2018
Journal Name
Osr Journal Of Pharmacy And Biological Sciences (iosr-jpbs)
Evaluation of toxicity in rats of Ruta chalepensıs L. extracts Growıng in Iraq
...Show More Authors

Evaluate the acute and chronic toxicity of Ruta Chalepensis aerial part aqueous extract used in folk medicine in Iraq in Albino Wistar male and female rats. The study of chronic toxicity at the doses 100, 300 and 600mg/kg body weight in male and female rats for 90 days, recorded no mortality. Treated animals showed a normal weight change compared with control. The parameters of male fertility showed a significant decrease in the weight of testis, epididymis and seminal vesicle as well as a reduction in the number and the motility of spermatozoids at treated groups by the doses 300 and 600 mg/kg body weight compared to control group.

Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Evaluation of some biochemical and immunological parameters changes in Iraq male with toxoplasmosis
...Show More Authors

A total of 33 Iraq male positive for Toxoplasmosis and Iraq male negative for Toxoplasmosis (controls) were studies to Evaluation of some biochemical and immunological parameters changes.The parameters included lipid profile such as (Cholesterol(C), Triglycerides(TG), High-Density Lipoprotein (HDL), Low-Density Lipoprotein (LDL) and very Low-Density Lipoprotein (VLDL) and complement component C3 and C4. The results revealed significant decrease in the total cholesterol, Triglycerides, LDL and non-significant in vLDL (129.96±1.63, 130.69± 2.80, 87.19±1.97, 29.24± 0.83 mg/dl respectively) and non-significant increase in HDL(24.22 ±0.62) mg/dl compared with control group(152.07± 1.63, 156.48± 6.55, 99.26 ±1.39, 31.49± 1.30 and 21.31±

... Show More
Preview PDF
Scopus (1)
Scopus
Publication Date
Sun Jun 03 2012
Journal Name
Baghdad Science Journal
Evaluation the Levels of Serum Hormones (Progesterone, Estradiol, and hCG) in Preeclamptic IraqiPregnancies
...Show More Authors

This study aimed to evaluate serum levels of steroid hormones and human chorionic gonadotropin (hCG) hormone in preeclamptic Iraqi pregnancies compared to those of healthy pregnancies.This study enrolled 120 pregnant women, divided into four groups:1. 30 healthy pregnant women.2. 37 pregnant women with mild preeclampsia3. 53 pregnant women with severe preeclampsia4. 90 pregnant women with preeclampsia Preeclamptic women and their severe cases but not mild cases had significantly (P<0.01) increased levels of serum hCG as compared with healthy pregnancies. By contrast, sera levels of estradiol were significantly (P<0.01) decreased in total preeclamptic groups and their severe cases but not in mild group as compared to healthy pregnant wome

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Apr 13 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Evaluation of IL-35 and hs-CRP in Iraqi Patients with Cardiovascular diseases
...Show More Authors

    Interleukin-35 (IL-35) is a novel anti-inflammatory of IL-12 family member cytokine. High sensitive C- reactive protein (hs-CRP) is a marker of inflammation disease. This study was obtained to estimate the concentrations of IL-35 and hs-CRP in cardiovascular diseases Iraqi patients. The study contained 79 subjects divided into two groups, 47 (21 male and 26 female) suffering from cardiovascular diseases and 32 as control group. The concentration of IL-35 and hs-CRP was measured by enzyme- linked immune sorbent assay (ELISA). The results revealed that the concentrations of IL-35 and hs-CRP are increased in patients group. IL-35 is strongly expressed in human advanced plaque and hs-CRP. Therefore these two biomarkers cou

... Show More
View Publication Preview PDF
Publication Date
Wed Nov 24 2021
Journal Name
Iraqi Journal Of Science
Evaluation of CD14 expression in Helicobacter pylori positive and Helicobacter pylori negative gastritis
...Show More Authors

Monocytes are considered a key mediator of inflammatory cytokine secretions during inflammation. This study evaluates CD 14 expression in gastritis tissue biopsies of H. pylori and none H. pylori gastritis. This cross-sectional study involved 60 gastritis patients that have been classified into H. pylori positive (n=30) and H. pylori negative (n=30). Formalin fixed paraffin embedded tissue blocks were sectioned and immune-peroxidase staining with anti-CD14, then compared between study groups and clinical parameters. The results showed a marked difference in the percentage of expression in mild and severe intensity of inflammation sub-groups, the results showed a higher percentage of CD14 immunoreactivity (18.29±5.84 vs. 10.2±3.89, p=0.

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Nov 25 2022
Journal Name
Baghdad Science Journal
Evaluation of Some Antioxidants and Oxidative Stress Tests in Iraqi Lung Cancer Patients
...Show More Authors

Vitamin K-dependent protein (VKDP) contributes to the development of lung cancer. The purpose of this research was to better understanding of the role of blood matrix Gla protein (MGP), VKDPs, Malondialdehyde (MDA), Superoxide dismutase (SOD) and Vitamin K (Vit K) in Iraqi patients with lung cancer before and after the first cycle of chemotherapy. Blood samples were collected from Al amal National Hospital for cancer treatment from October 2021 to May 2022, and a total of 80 samples were collected, divided into two groups (40 patient before taking a chemotherapy and 40 patients after taking chemotherapy), ranging in age from 20 to 45 years old. The results showed that although there were highly statistically significant differences in MD

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Evaluation of ELectrolytes in Adult Patients with Acute Leukemia before and after Chemotherapy
...Show More Authors

Abstract:Leukemia is a cancer of early blood forming cells. Most of them are cancers of white blood cells , however some leukemias start in other blood cell types.Electrolytes have modulatory effects on several biological mechanisms in the body namely as stabilizers,element of structures, essential element for hormonal function and also co-factors for a number of enzymes.In this study serum electrolytes levels were measured in patients with acute leukemia (AL) disorders before and after chemotherapy(anthracycline, doxorubicin, cytarabine ,prednisone, vincristine and doxorubicin) during one month and compared with that of control group. Blood samples were obtained from (43) patients (28 males and 15 females) aged (15-55)years;juset before an

... Show More
View Publication Preview PDF
Crossref