A5010197883- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Multicomponent Synthesis of Heterocycles
- Bioactive Compounds and Antitumor Agents
- HER2/EGFR in Cancer Research
- Inorganic and Organometallic Chemistry
- Various Chemistry Research Topics
- Synthesis of Tetrazole Derivatives
- Synthesis and Characterization of Heterocyclic Compounds
- Chemistry and Chemical Engineering
- Neuroscience and Neuropharmacology Research
- Quinazolinone synthesis and applications
- Click Chemistry and Applications
- Synthesis and pharmacology of benzodiazepine derivatives
Al-Azhar University
2004-2022
Al-Azhar University
2021
Delta University for Science and Technology
2015-2020
A series of hybrid triazoloquinoxaline-chalcone derivatives 7a-k were designed, synthesized, fully characterized, and evaluated for their cytotoxic activity against three target cell lines: human breast adenocarcinoma (MCF-7), colon carcinoma (HCT-116), hepatocellular (HEPG-2). The preliminary results showed that some these chalcones like 7b-c, 7e-g exhibited significant antiproliferative effects most the lines, with selective or non-selective behavior, indicated by IC50 values in 1.65 to...
Abstract Targeting the epidermal growth factor receptors (EGFRs) with small inhibitor molecules has been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo[3,4‐ d ]pyrimidine is versatile scaffold that exploited for developing anticancer agents. On basis of fragment‐based drug discovery, considering essential pharmacophoric features potent EGFR tyrosine kinase (TK) inhibitors, herein, we report design and synthesis new hybrid pyrazolo[3,4‐ linked diverse fragments...
The resistance of pathogenic microbes to currently available antimicrobial agents has been considered a global alarming concern.
In continuation of our previous work on the design and synthesis topoisomerase II (Topo II) inhibitors DNA intercalators, a new series quinoxaline derivatives were designed synthesized. The synthesized compounds evaluated for their cytotoxic activities against panel three cancer cell lines (Hep G-2, Hep-2, Caco-2). Compounds 18b, 19b, 23, 25b, 26 showed strong potencies all tested with IC50 values ranging from 0.26 ± 0.1 to 2.91 µM, comparable those doxorubicin (IC50 0.65 0.81 µM). most...
Abstract Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline derivatives as DNA gyrase inhibitors. The preliminary activity was assessed against a panel pathogenic microbes including Gram‐positive bacteria ( Streptococcus pneumoniae Bacillus subtilis ), Gram‐negative Pseudomonas aeruginosa Escherichia coli fungal strains Aspergillus fumigatus , Syncephalastrum racemosum Geotrichum candidum Candida albicans ). Compounds that revealed best were subjected to...
2-([1,2,4]Triazolo[4,3-a]quinoxalin-4-ylthio)acetic acid hydrazide (10) was used as a precursor for the syntheses of novel quinoxaline derivatives with potential anticonvulsant properties. The newly synthesized compounds have been characterized by IR, (1)H NMR, and mass spectral data followed elemental analysis. evaluation carried out eleven using metrazol induced convulsions model phenobarbitone sodium standard. Among this set tested compounds, two them (14, 15b) showed best activities.
A series of 3-substituted 6-methoxy-1H-pyrazolo [3,4-b]quinoline derivatives was synthesized by treating 6-methoxy-1H-pyrazolo[3,4-b]quinolin-3-amine (6) with different acid anhydrides including succinic anhydride, maleic anhydride and phthalic anhydride. Also, a 3-heteroaryl-2-chloro-6-methoxyquinolines prepared through 1,3-dipolar cycloaddition bi-nucleophiles hydrazine hydrate, hydroxylamine hydrochloride, thiourea, guanidine urea metformin hydrochloride to the chalcone derivative...
Vilsmeier formylation of acetanilide I followed by treatment with hydroxylamine produced2-chloroquinoline-3-carbonitrile II that was condensed different amines to give 2-substituted aminoquinolines-3-carbonitriles III. Treatment thiourea yielded 2-mercaptoquinoline-3-carbonitrile IV, which converted its potassium salt V wascondensed some chloroacetate esters produce thioquinoline-3-carbonitriles VI. Hydrazinolysis or IV gave 1H-pyrazolo[3,4-b]quinolin-3-ylamine VII.Condensation VII aryl...
A series of new 6-methoxyquinoline-3-carbonitrile derivatives were synthesized using a variety synthetic routes. The newly compounds have been characterized by IR, 1H NMR, and mass spectral data followed elemental analysis. All the evaluated for their in-vitro antimicrobial activity against Streptococcus pneumonia Bacillus subtilis as examples Gram-positive bacteria, Pseudomonas aeruginosa Escherichia coli Gram-negative Aspergillus fumigatus, Syncephalastrum racemosum, Geotriucum candidum...
Background: Benzodiazepines (BDZs) are predominantly prescribed as sedatives, anxiolytics, and anticonvulsants throughout the world they act on GABAA receptor.Objective: New 1,4-BDZ analogues have been designed synthesized to be evaluated for their anticonvulsant activity.Methods: The newly compounds examined by Maximal electroshock seizure (MES) test, subcutaneous pentylenetetrazol (scPTZ) rotarod neurotoxicity test.Docking study was performed justify activity.Results: most active compound...