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 Oct 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
New Green Modalities of Flow Injection Technology for Assaying Anti-Allergic Drugs in Pharmaceutics and Biological Samples
...Show More Authors

A new approach and the developed FIA technique with many advantages (economic, fast, simple, accurate, and high throughput) are used to determine the decongestant drugs (Phenylephrine.HCl, Oxymetazoline.HCl) in biological samples, pharmaceutical formulations, and pure samples via continuous flow injection technique by oxidative coupling reaction, where the method depends on the interaction of the decongestant drug with organic reagents to produce colored compounds, where Phenylephrine reacts with 4-AAP at λmax503 nm to produce a red compound, and the Beer’s law range of 10-600 μg.mL-1 . As for Oxymetazoline, it reacts with DNPH at λmax 631nm to produce a green compound with a linear dynamic range of

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Jun 01 2012
Journal Name
Pharmacie Globale
Synthesis and microbiological study of new sulfonamides
...Show More Authors

In contrast to the classical antibacterial sulfa drugs that are unsubstituted or monosubstituted, our newly synthesized analogs were designed to obtain sulfonamide moiety containing disubstituted hetero nitrogen atom. These compounds were formed successfully by chlorosulfonation of acetanilide and the product was treated with different cyclic amines and finally amide hydrolysis was necessary to get agents that were analyzed for IR, UV, CHN, melting points and solubility. At last, we studied their antibacterial activity on certain types of bacteria and we noticed the inactivity due to possible steric factor. Principly, this means these products have no inhibiting action against the used microbes.

Publication Date
Wed Jun 04 2008
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and characterization of new ligand c
...Show More Authors

In the present paper we report the synthesis of a new ligand [HL][(2-1-[(2-hydroxy-benzylidene)-hydrazono]-ethyl) benzene-1, 3, 5-triol and its complexes with (Mn", Fe", Cd", and Hg") The ligand was prepared in two steps. In the first step a solution of salicylaldehyed in methanol reacted under reflux with hydrazinemonohydrate to give an intermediate compound which reacted in the second step with 2, 4, 6-trihydroxidernonohydrate giving the tientioned ligand. The complexes were synthesis by direct reaction of the corresponding metal chloride with ligand. The ligand and the complexes have been characterized by spectroscopic methods [" H NMR, IR, UV-Vis,, atomic absorption], HPLC microanalysis along with conductivity measurements. From the abo

... Show More
Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis of New Amide and ThioUrease Compounds.
...Show More Authors

The reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.

View Publication Preview PDF
Crossref
Publication Date
Tue Feb 02 2021
Journal Name
International Journal Of Pharmaceutical Research
Antimicrobial Evaluation of Some New Synthesized NHydroxy Phthalimide Derivatives
...Show More Authors

In this work, N-hydroxy phthalimide derivatives (NHPID) were synthesized from the nucleuphilic substitution reactions of (NHPI) with different halides (alkyl halides, sulfonyl halides, benzoyl halides and benzyl halides). The products were distinguished using FTIR spectrum and Nuclear magnetic resonsnce (1H-NMR and 13CNMR), in addition to other characteristic methods such as sodium fution for sulfur determination. followed by measuring antibacterial (with different types of gram positive/gram negative bacteria) and antifungal activities of these compounds.

View Publication
Crossref (1)
Crossref
Publication Date
Sat Jan 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Modification, Characterization of New Thiazolidinone and Oxazolidinone Derived from Levofloxacin and Evaluation of Anti-Oxidant
...Show More Authors

The research study included the synthesis of a new series of heterocyclic derivatives containing the antibiotic Levofloxacin. The first way provides for the reaction of  Levofloxacin with thionyl chloride in benzene as a solvent to give an acid chloride derivative. A new class of acid hydrazide synthesized from Levofloxacin was studied. Schiff bases were produced via the reaction of acid hydrazide with substituted aromatic ketones in methanol. The next stage involved the response of Schiff bases with thioglycolic acid and mono chloroacetic acid in DMF to produce derivatives of the antibiotic levofloxacin that have five heterocyclic members, including the derivatives thiazolidine-4-one and oxazolidine-5-one. The FTIR, 1HNMR, a

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jan 01 2020
Journal Name
Annals Of Tropical Medicine And Public Health
Synthesis and characterization of new phthalimide with 6- mercaptopurine or 2- aminothiazole conjugate used dithiocarbamate spacer as anticancer agents
...Show More Authors

View Publication
Crossref
Publication Date
Wed Nov 02 2022
Journal Name
Neuroquantology
Inhibition activity of mucilage prepared of Salvia hispanica as anti filamentary and anticancer
...Show More Authors

An International Publisher for Academic and Scientific Journals The mucilage of white and black chia seeds were extracted and determining their contents of bioactive compounds such as tannins, glycosides, flavonoids, phenols, and studying their activity as anti-filamentary and anticancer. Results showed that tannins exist in white chia seeds with 35%while it is 38% in black seeds, flavonoids represent 0.98mg/ml in white chia seeds and 1.5 mg/ml for black seeds. Both kinds of seeds showed anti-filamentaryactivity, the inhibition ratio was 86.5% for white seeds and 97.3% for black seeds. Chia black seeds showed anticancer activity and the inhibition of the tumor muscle cell line ratio (GI%) was 34.8% at 50mg/ml concentration and 88.4%

... Show More
View Publication Preview PDF
Publication Date
Tue Oct 31 2023
Journal Name
Malaysian Journal Of Science
SYNTHESIS, PHYSICOCHEMICAL ELUCIDATION AND BIOLOGICAL SCREENING STUDY OF NEW LIGAND DERIVED FROM 5,6-O-ISO PROPYLIDENE-L-ASCORBIC ACID AND ITS METAL(II) COMPLEXES
...Show More Authors

A simple chemistry method approach was used to synthesise new ligand derivate from L-ascorbic acid and its complexes. All of them were water-soluble and are used quite extensively in the medical and pharmaceutical fields. This study synthesised the new ligand derivative from L-ascorbic acid-base using the following steps: A 5,6-O-isopropylidene-L-ascorbic acid was prepared by reacting dry acetone with L-ascorbic acid followed by reacting it with trichloroacetic acid to yield [chloro(carboxylic)methylidene]-5,6-O-isopropylidene-L-ascorbic acid in the second stage. In the third stage, the derivative was reacted with (methyl(6-methyl-2-pyridylmethyl)amine to create a new ligand (ONMILA). This novel ligand was identified using a number

... Show More
View Publication
Scopus (2)
Crossref (1)
Scopus Crossref
Publication Date
Mon Jan 01 2018
Journal Name
Journal Of Pharmacy Research
Design and in vitro characterization of bisacodyl as a hollow-type suppositories
...Show More Authors