A5080556228- Synthesis and biological activity
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
- Quinazolinone synthesis and applications
- Click Chemistry and Applications
- Crystallization and Solubility Studies
- Computational Drug Discovery Methods
- X-ray Diffraction in Crystallography
- Melanoma and MAPK Pathways
- Inflammatory mediators and NSAID effects
- Synthesis and Characterization of Heterocyclic Compounds
- Essential Oils and Antimicrobial Activity
- Natural product bioactivities and synthesis
- Advancements in Transdermal Drug Delivery
- Bioactive Compounds and Antitumor Agents
- Drug-Induced Hepatotoxicity and Protection
- Lung Cancer Treatments and Mutations
- Cytokine Signaling Pathways and Interactions
- Protein Degradation and Inhibitors
- Protein Kinase Regulation and GTPase Signaling
- HER2/EGFR in Cancer Research
- Nanoparticle-Based Drug Delivery
- Liver Disease Diagnosis and Treatment
- Pharmacogenetics and Drug Metabolism
- Eicosanoids and Hypertension Pharmacology
Jouf University
2018-2025
Nahda University
2018-2020
A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using 1H NMR, 13C elementary analyses. Using as a reference, compounds 1–21 were screened in vitro against Gram-positive bacterial strains such Staphylococcus aureus Bacillus subtilis Gram-negative Escherichia coli Pseudomonas aeruginosa. As result, many the examined had antibacterial activity equivalent to test bacteria. Compounds 2–6, oxadiazole derivatives,...
A series of 1,3,4-oxadiazole-1,2,3-triazole hybrids bearing different pharmacophoric moieties has been designed and synthesized. Their antiproliferative activity was evaluated against four human cancer cell lines (Panc-1, MCF-7, HT-29, A-549) using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The preliminary test displayed that most active compounds, 6d, 6e, 8a-e, suppressed growth (GI50 = 0.23-2.00 µM) comparably to erlotinib 0.06 µM). Compounds 8a-e...
DNA gyrase and topoisomerase IV show great potential as targets for antibacterial medicines. In recent decades, various categories of small molecule inhibitors have been identified; however, none effective in the market. For first time, we developed a series disalicylic acid methylene/Schiff bases hybrids ( 5a-k ) to act agents targeting IV. The findings indicated that new 5f-k exhibited significant activity against Gram-positive Gram-negative bacteria, with efficacy ranging from 75% 115%...
The investigation of novel EGFR and BRAF
Bacterial resistance is spreading in an alarming manner, outpacing the rate of development new antibacterial agents and surging need for effective alternatives. Prenylated flavonoids are a promising class natural antibiotics with reported activity against wide range resistant pathogens. Here, large library (1718 structures) was virtually screened potential candidates inhibiting B-subunit gyrase (Gyr-B). Twenty-eight candidates, predominated by prenylated flavonoids, appeared as hits. Six...
Abstract As dual EGFR and BRAF V600E inhibitors, 2‐(3‐cyano‐4,6‐bis(aryl)‐2‐oxo‐1,2‐dihydropyridine‐1‐yl)‐ N ‐(4‐cinnamoylphenyl) acetamide derivatives 8–20 were developed. Compounds 8, 12 , 13 showed strong antiproliferative activity when the target compounds synthesized tested in vitro against four cancer cell lines. These hybrids have a inhibition on according to studies. The was inhibited by with IC 50 values between 89 110 nM, which equivalent those of erlotinib (IC = 80 nm). Compound...
In this article, we display on the synthesis and biological evaluation of a new series thiazolylpyrimidine 3a-l thiazolidinylpyrimidine derivatives 5a-e. The structures compounds were confirmed by using different spectral techniques including NMR, IR, mass spectroscopy in addition to elemental analyses. cell viability was assessed against normal human mammary gland epithelial (MCF-10A) line. Data revealed that none examined exhibited cytotoxic effects, for at 50 µM greater than 87%....
Geraniol (GER) is a plant-derived acyclic isoprenoid monoterpene that has displayed anti-inflammatory effects in numerous vivo and vitro models. This study was therefore designed to evaluate the antiarthritic potential of GER complete Freund's adjuvant (CFA)-induced inflammatory arthritis (IA) model rats. IA induced by intraplantar injection CFA (0.1 mL), week after administration, rats were treated with various doses methotrexate (MTX; 1 mg/kg) or (25, 50, 100 mg/kg). Treatments given on...
DNA gyrase is a promising target for antibacterial agents. Several classes of small-molecule inhibitors have been discovered in recent decades, but none these reached the market. We designed small library 1,2,4-oxadiazole/pyrrolidine hybrids with mid nanomolar inhibitory and potent activities against topoisomerase IV. Compounds 9, 15, 16, 19, 21 inhibited Escherichia coli to similar extent as reference compound, novobiocin, values ranging from 120 nM 270 nM. Compound 16 was one most...