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
Sat Aug 01 2020
Journal Name
Research Journal Of Pharmacy And Technology
Evaluation of in vivo and in vitro protective effects of quercetin on lipopolysaccharide-induced inflammation and cytotoxicology
...Show More Authors

Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT

... Show More
Publication Date
Sat Mar 01 2014
Journal Name
International Journal For Sciences And Technology
Preparation of Carboxy Methylated mPEG-Block-(4-Dodecyl Anilide) Copolymers and Their Visco Metric and Surface Tension Properties in THF
...Show More Authors

Preparation of Carboxy Methylated mPEG-Block-(4-Dodecyl Anilide) Copolymers and Their Visco Metric and Surface Tension Properties in THF

Publication Date
Fri Jun 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and in Vitro Evaluation for Different Types of Ondansetron Hydrochloride Transdermal Patches
...Show More Authors

This research aims to develop transdermal patches of Ondansetron hydrochloride (OSH) with different types of polymers, ethyl cellulose and, polyvinyl pyrrolidone k30 in a ratio (3:0.5,3:1,3:2,2:1,1:1) with propylene glycol 20%w/w as a plasticizer. Prepared transdermal patches were evaluated for physical properties. The compatibility between the drug and excipients was studied by Differential scanning calorimetry (DSC), where there is no interaction between the drug and polymers. From the statistical study, there is a statistical difference between all the prepared formulations p<0.05. In-vitro Release study of transdermal patches was performed by using a paddle over the disc. The release profile of OSH follow

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Thu Jun 01 2023
Journal Name
Materials Chemistry And Physics
In-vitro antibacterial, cytotoxicity, and anti-prostate cancer effects of gold nanoparticles synthesized using extract of desert truffles (Tirmania nivea)
...Show More Authors

Herein, a cost-effective bio approach using extract derived from desert truffles (Tirmania nivea) is utilized to synthesize gold nanoparticles (AuNPs). AuNPs were thoroughly investigated using UV–vis, XRD, SEM, and TEM analyses. It was shown that nanoparticles had an fcc structure with a smooth spherical surface, an average diameter of 9.44 ± 0.26 nm, and an SPR band observed at 548 nm. Investigations were conducted on AuNPs' antibacterial and anti-cancer properties of prostate cancer cells. The findings suggest that AuNPs showed better antibacterial effects against S. aureus compared to E. coli, P. aeruginosa, and K. pneumoniae. AuNPs’ combination with antibiotics demonstrated a synergistic effect with significant antibacterial activi

... Show More
View Publication
Scopus (22)
Crossref (15)
Scopus Clarivate Crossref
Publication Date
Sun Mar 06 2022
Journal Name
Al–bahith Al–a'alami
Semiotic criteria for analyzing religious symbols in press reports Qantara news site as a model
...Show More Authors

The report includes a group of symbols that are employed within a framework that gives a language of greater impact. This research discusses the problem of the semiotic employment of religious symbols in press reports published in the electronic press across two levels: Reading to perceive the visual message in its abstract form, and the second for re-understanding and interpretation, as this level gives semantics to reveal the implicit level of media messages through a set of semiotic criteria on which it was based to cut texts to reach the process of understanding and interpretation.

The report includes a group of symbols that are employed within a framework that gives a language of greater impact. This research discusses the p

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Oct 28 2023
Journal Name
Baghdad Science Journal
Small Nuclear RNA 64 (snoRNA64): A novel Tumor Biomarker for Pancreatic Cancer
...Show More Authors

The pancreatic ductal adenocarcinoma (PDAC), which represents over 90% of pancreatic cancer cases,
has the highest proliferative and metastatic rate in comparison to other pancreatic cancer compartments. This
study is designed to determine whether small nucleolar RNA, H/ACA box 64 (snoRNA64) is associated with
pancreatic cancer initiation and progression. Gene expression data from the Gene Expression Omnibus (GEO)
repository have shown that snoRNA64 expression is reduced in primary and metastatic pancreatic cancer as
compared to normal tissues based on statistical analysis of the in Silico analysis. Using qPCR techniques,
pancreatic cancer cell lines include PK-1, PK-8, PK-4, and Mia PaCa-2 with differ

... Show More
View Publication Preview PDF
Scopus (4)
Crossref (3)
Scopus Crossref
Publication Date
Sat Feb 18 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Preparation and In-Vitro Evaluation of Floating Oral In- Situ Gel of Montelukast Sodium (Conference Paper) #
...Show More Authors

Publication Date
Sun Apr 07 2013
Journal Name
Journal Of Educational And Psychological Researches
skills and its relationship to the with concept of self in social The chidren kindergarten age (4-6) years
...Show More Authors

 The interest in Multi social skills and self-concept is extremely  important for many of the scholars of education and psychology has taken a great deal in their writings and their interests as they see that social skills training is to make sure of the same, and that whenever enable the individual from acquiring social skills whenever asserted itself.The research aims know social skills and self-concept and their relationship to the children Riyadh age (4-6 years), and the research sample consisted of(200) boys and girls from kindergarten in the city of Baghdad Bjanbey Rusafa second and Karkh second.And to the objectives of the research realized the researcher has built two measures of social skills a

... Show More
View Publication Preview PDF
Publication Date
Wed Dec 30 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Association of Retinol Binding Protein- 4 (RBP4) with Glycemia, Dyslipidemia, Hypertension, and Obesity in Type 2 Diabetic Iraqi Patients
...Show More Authors

Abstract:

Background: Retinol binding protein 4 (RBP4), an adipokine that participate in a lipid metabolism or insulin resistance through a complex regulatory network. Recently, RBP4 was reported to be associated with many cardiovascular diseases (CVDs) risk factors in patients of type 2 diabetes mellitus (T2DM). This study aims to study the correlation of  serum RBP4 with some markers of glycemic control, dyslipidemia, hypertension and obesity in T2DM Iraqi patients.

Subjects and Methods: one hundred fifty participants were enrolled in this coss-sectional study, 120 of participants were T2DM patients and 30 were apparently healthy individuals to serve as control gro

... Show More
View Publication Preview PDF
Scopus (14)
Crossref (1)
Scopus Crossref
Publication Date
Wed Mar 01 2023
Journal Name
Journal Of Applied Spectroscopy
Spectrophotometric Method for the Determination of Naphazoline Nitrate in Bulk and Pharmaceutical Preparations by Using 1,2-Naphthoquinone-4-Sulfonate
...Show More Authors

View Publication
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref