Preferred Language
Articles
/
nBeILZIBVTCNdQwCLqdz
New Niflumic Acid Derivatives as EGFR Inhibitors: Design, Synthesis, In silico Studies, and Anti-proliferative Assessment
...Show More Authors
Background:

1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.

Objectives:

To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.

Methods:

The designed compounds were synthesized using conventional organic synthesis methods. The antitumor activities of the new NF derivatives against HepG2 hepatocellular carcinoma and A549 non-small cell lung cancer cell lines were assessed in vitro via MTT assay, flow cytometry, RT-PCR, as well as via molecular docking studies.

Results:

The cytotoxicity results indicated that the newly synthesized NF derivatives were cytotoxic against the two cancer cell lines, with compound 6 being the most cytotoxic, achieving the lowest IC50 concentration. Furthermore, compound 6 targeted EGFR tyrosine kinase leading to cell cycle arrest at the G2/M cell cycle phase and induction of apoptosis. The in vitro biological investigation results matched those of the molecular docking analysis. In conclusion, the new NF derivatives, specifically compound 6, exhibited favorable pharmacokinetic features and are promising EGFR tyrosine kinase inhibitors.

Conclusion:

A series of niflumic acid derivatives (3, 4A-E, 5, and 6) were successfully created, and FT-IR, 1H, 13CNMR, and HRMS were used to confirm their chemical structures. According to molecular docking studies, compounds 3, 5, and 6 have the highest docking scores (ΔG), and most tested compounds have a good pharmacokinetic profile. Results of compound 6 in vitro antitumor activities showed that it is a promising EGFR tyrosine kinase inhibitor.

Scopus Clarivate Crossref
View Publication
Publication Date
Fri Sep 01 2023
Journal Name
Journal Of Molecular Structure
Synthesis, spectral studies, DFT, biological evaluation, molecular docking and dyeing performance of 1-(4-((2-amino-5-methoxy)diazenyl)phenyl) ethanone complexes with some metallic ions
...Show More Authors

Scopus (60)
Crossref (52)
Scopus Clarivate Crossref
Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Physiological and Immunological Assessment in Infertile Women Undergoing In-vitro Fertilization
...Show More Authors

All the available reports on the issue of infertility confirmed the increase in this population problem worldwide. Although the accurate estimate of the number of infertile people is due to several reasons, including the discrepancy in the true definition of infertility (whether it extends for one, two or five years of failed pregnancy attempts), as well as the great discrepancy in the size of the selected population groups (large population sample size versus epidemiological studies) and defining the category that diagnosed included (individuals, women, or couples). The goal of today’s IVF program is to obtain high-quality embryos with high efficiency in development, which leads to an increase in live birth rates.

View Publication Preview PDF
Scopus Crossref
Publication Date
Sat Jun 18 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Some Pro and Anti-Inflammatory Cytokines in Children with Tonsillitis and their Correlations with Vitamin D Deficiency
...Show More Authors

Inflammation of the tonsils could be described as acute tonsillitis, mainly due to infection. Recurrent tonsillitis could be defined as 3-7 episodes during the first 3 years of age. Vitamin D, which is a neuro-hormone with pleiotropic biological activities may modulate the immune response by alleviation, and stimulation of Th1 and Th2 cell proliferation, respectively, that influence the stimulation, synthesis, and secretion of both pro and anti-inflammatory cytokines. In this study we aimed to shed light on the levels of vitamin D in children with different episodes of tonsillitis in association with levels of interleukins (TNFα, IL-2, IL-4, IL-10). Blood samples were collected from 48 participants in 3 groups: control, acute tonsilliti

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (4)
Scopus Crossref
Publication Date
Mon Jun 15 2020
Journal Name
Journal Of Baghdad College Of Dentistry
Association between anti-CMV IgG and salivary levels of IL‐6 and TNF-α in chronic periodontitis
...Show More Authors

Background: Periodontitis is an infection attributable to multiple infectious; it causes an interrelated cellular and humoral host immune responses. Recent reports have indicated that human cytomegalovirus (HCMV) may contribute to pathogenesis of periodontitis. The HCMV can stimulate the release of cytokines from inflammatory and non-inflammatory cells and weaken the periodontal immune defense. This study aimed to reveal the presence of anti-CMV IgG, and determine the levels of IL‐6 and TNF-α and to correlate the presence of cytomegalovirus (CMV) with cytokines levels. Materials and Methods: Forty patients with chronic periodontitis and 40 healthy control subjects (their age and sex were matched with the patients) were involved

... Show More
View Publication Preview PDF
Scopus (10)
Crossref (7)
Scopus Crossref
Publication Date
Sun Jan 14 2018
Journal Name
Journal Of Engineering
The effect of Laser Shock Peening on Fatigue Life Using Pure Water and Hydrofluoric Acid As a Confining Layer of Al – Alloy 7075-T6
...Show More Authors

Laser shock peening (LSP) is deemed as a deep-rooted technology for stimulating compressive residual stresses below the surface of metallic elements. As a result, fatigue lifespan is improved, and the substance properties become further resistant to wear and corrosion. The LSP provides more unfailing surface treatment and a potential decrease in microstructural damage. Laser shock peening is a well-organized method measured up to the mechanical shoot peening. This kind of surface handling can be fulfilled via an intense laser pulse focused on a substantial surface in extremely shorter intervals. In this work, Hydrofluoric Acid (HF) and pure water as a coating layer were utilized as a new technique to improve the properti

... Show More
View Publication Preview PDF
Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Synthesis and Characterization of N-((6-substituted - Benzothiazol-2-Y)succunamic acid.3-(6-substituted-benzothiazol-2-Y1)-Carbamoyl Prorionyl Chloride and study of thier Biological effects
...Show More Authors

Twelve N-(6-sustirured benzothanol-2-y1) succinamic acids and 3-(6-substitted benzonathol-2-y1)-carbamoyl propionyl chloride were synthesized in good yields from reaction of benzonathol2-yl)

View Publication Preview PDF
Publication Date
Wed May 07 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
...Show More Authors

The [2-hydroxy -1,2-diphynel-ethanone oxime] was reacted with 1,2- dichloroethan to give the new ligand [H2L].this ligand was reacted with some metal ions (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) in methanol as a solvent to give a series of new (1:1)complexes of the general formula [ M(HL)]Cl ,( where : M= Co(II),Ni(II),Cu(II),Zn(II) and Cd(II)) are isolated All compounds have been characterized by spectroscopic methods [ I.R , U.V -Vis ] atomic absorption . Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure.

Publication Date
Tue Jan 15 2008
Journal Name
Journal Of Kerbala University
Synthesis and Characterization of New Ligand type N2O2 and its complexes with (Co(II),Ni(II),Cu(II),Zn(II) and Cd(II) ions
...Show More Authors

The [2-hydroxy-1, 2-diphynel-ethanone oxime] was reacted with 1, 2-dichloroethan to give the new ligand [H2L]. this ligand was reacted with some metal ions (Co (II), Ni (II), Cu (II), Zn (II) and Cd (II) in methanol as a solvent to give a series of new (1: 1) complexes of the general formula [M (HL)] Cl,(where: M= Co (II), Ni (II), Cu (II), Zn (II) and Cd (II)) are isolated All compounds have been characterized by spectroscopic methods [IR, UV-Vis] atomic absorption. Chloride content along with conductivity measurements. From the above data the proposed molecular structure for (Co, Cu, Ni, Zn and Cd) complexes adopting a tetrahedral structure

Publication Date
Thu Jul 02 2015
Journal Name
Diyala Journal For Pure Sciences
Synthesis and characterization of new bidentate chalcone ligand type (NO) and its MnІІ, CoІІ, NiІІ and CuІІ complexes with study of their antibacterial activity
...Show More Authors

The aim of the work is synthesis and characterization of new bidentate chalcone ligand type (NO):[(E)-1-(3-aminophenyl)-3-(4-chlorophenyl) prop-2-en-1-one] [H2L], from the reaction of 3-amino acetophenone with 4-chloro benzaldehyde to produce the ligand [H2L], the reaction was carried out in ethanol as a solvent under stirring. The prepared ligand [H2L] was characterized by FT-IR, UV-Vis spectroscopy, 1H, 13C-NMR spectra, Mass spectra, (C.H.N) and melting point. The complexes of ligand [H2L] were prepared with metal ion M(Π).Where M(Π) = (Mn ,Co ,Ni and Cu) at reflux ,using ethanol as a solvent and KOH as a base with molecular formula [M (H2L)2] +2 where: H2L= (C15H12NOCl). All the complexes were characterized by spectroscopic met

... Show More
Publication Date
Sat Jun 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis and Characterization of New Ligand for β-enaminone and its Mixed Ligand Complexes with Some Metal Ions and Evaluation of their Biological Activity
...Show More Authors

The synthesized ligand (3-(2-amino-5-(3,4,5-tri-methoxybenzyl)pyrimidin-4-ylamino)-5,5-dimethylcyclohex-2-enone] [H1L1] was characterized via fourier transform infrared spectroscopy (FTIR), 1H, 13C – NMR, Mass spectra, (CHN analysis), UV-vis spectroscopic approaches. Analytical and spectroscopic techniques like chloride content, micro-analysis, magnetic susceptibility UV-visible, conductance, and FTIR spectra were used to identify mixed ligand complexes. Its (ML13ph) mixed ligand complexes [M= Co (II), Ni (II), Cu (II), Zn (II), and Cd (II); (H1L1) = β-enaminone ligand=L1 and (3ph) =3-aminophenol= L2]. The results demonstrate that the complexes are produced with a molar ratio of M: L1:L2 (1:1:1). To generate the appropriate compl

... Show More
View Publication
Scopus (3)
Crossref (1)
Scopus Crossref