A5072315789- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Computational Drug Discovery Methods
- Analytical Chemistry and Chromatography
- Analytical Methods in Pharmaceuticals
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- SARS-CoV-2 and COVID-19 Research
- Bioactive Compounds and Antitumor Agents
- COVID-19 Clinical Research Studies
- Organoselenium and organotellurium chemistry
- Pharmacological Effects of Natural Compounds
- Essential Oils and Antimicrobial Activity
- Lung Cancer Treatments and Mutations
- Phytochemistry and Biological Activities
- Analytical Chemistry and Sensors
- Drug Transport and Resistance Mechanisms
- Antibiotics Pharmacokinetics and Efficacy
- Phenothiazines and Benzothiazines Synthesis and Activities
- RNA Interference and Gene Delivery
- Inflammatory mediators and NSAID effects
- Phytochemistry and Bioactivity Studies
- HER2/EGFR in Cancer Research
- Pharmacological Effects and Assays
Port Said University
2021-2025
National Organization for Drug Control and Research
2012-2017
Mansoura University
1990
The discovery of drugs capable inhibiting SARS-CoV-2 is a priority for human beings due to the severity global health pandemic caused by COVID-19. To this end, repurposing FDA-approved such as NSAIDs against COVID-19 can provide therapeutic alternatives that could be utilized an effective safe treatment anti-inflammatory activity also advantageous in COVID-19, it was found responsible provoking inflammatory cytokine storms resulting lung damage. In study, 40 were evaluated through molecular...
The global prevalence of COVID-19 disease and the overwhelming increase in death toll urge scientists to discover new effective drugs. Although drug discovery process is a challenging time-consuming, fortunately, plant kingdom was found have many active therapeutics possessing broad-spectrum antiviral activity including those candidates against severe acute respiratory syndrome coronaviruses (SARS-CoV). Herein, nine traditional Chinese medicinal constituents from different origins...
Cancer is a leading cause of death worldwide and its incidence unfortunately anticipated to rise in the next years. On other hand, vascular endothelial growth factor receptor 2 (VEGFR-2) highly expressed tumor-associated cells, where it affects tumor-promoting angiogenesis. Therefore, VEGFR-2 considered one most promising therapeutic targets for cancer treatment. Furthermore, some FDA-approved benzimidazole anthelmintics have already shown potential anticancer activities. repurposing them...
The global breakout of COVID-19 and raised death toll has prompted scientists to develop novel drugs capable inhibiting SARS-CoV-2. Conducting studies on repurposing some FDA-approved glucocorticoids can be a promising prospective for finding treatment COVID-19. In addition, the use anti-inflammatory drugs, such as glucocorticoids, is pivotal step in critical cases COVID-19, they provoke an inflammatory cytokine storm, damaging lungs. this study, 22 were identified through silico (molecular...
Hydroxyethylamine and hydroxyethylene moieties of β-blockers exert potential SARS-CoV-2 inhibitory effects: rational-based design in silico , vitro SAR Studies.
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 a non-nucleoside selective telomerase inhibitor; however, it experiences ineligible pharmacokinetics. Herein, we aimed to design new BIBR1532-based analogues as promising inhibitors. Therefore, two novel series of pyridazine-linked cyclopenta[b]thiophene (8a-f) and tetrahydro-1-benzothiophene (9a-f) were synthesized. A quantitative real-time polymerase chain reaction was utilized investigate the inhibitory activity...
In this article, 34 anticoagulant drugs were screened in silico against the main protease (Mpro) of SARS-CoV-2 using molecular docking tools. Idraparinux, fondaparinux, eptifibatide, heparin, and ticagrelor demonstrated highest binding affinities towards Mpro. A dynamics study at 200 ns was also carried out for most promising anticoagulants to provide insights into dynamic thermodynamic properties compounds. Moreover, a quantum mechanical conducted which helped us attest some findings....
Herein, a series of N'-benzylidene-3,4-dimethoxybenzohydrazide derivatives were designed and synthesised to target the multidrug efflux pump (MATE). The antibacterial activities screened against S. aureus, Acinetobacter, typhi, E. coli, P. aeruginosa, whereas their antifungal C. albicans. Compounds 4a, 4h, 4i showed most promising activities. Moreover, compounds 4h being broader superior members regarding antimicrobial effects selected be further evaluated via in vivo testing using...
The global outbreak of the COVID-19 pandemic provokes scientists to make a prompt development new effective therapeutic interventions for battle against SARS-CoV-2. A series
Novel cyclopentaquinoline derivatives as promising DNA intercalators, topoisomerase II inhibitors, and apoptotic inducers.
Topoisomerases II are ubiquitous enzymes with significant genotoxic effects in many critical DNA processes. Additionally, epidermal growth factor receptor (EGFR) plays pivotal role tumour and angiogenesis. A novel series of naphtho[2',3':4,5]thiazolo[3,2-a]pyrimidine hybrids have been designed, synthesised evaluated for their topo IIα/EGFR inhibitory apoptotic inducer activities. Cytotoxicity the was against MCF-7, A549 HCT-116 cell lines. Of hybrids, 6i, 6a 6c experienced superior cytotoxic...
Microbial DNA gyrase is regarded as an outstanding microbial target. Hence, 15 new quinoline derivatives (5-14) were designed and synthesized. The antimicrobial activity of the afforded compounds was pursued via in vitro approaches. investigated displayed eligible MIC values, particularly against G-positive Staphylococcus aureus species. Consequently, S. supercoiling assay performed, using ciprofloxacin a reference control. Obviously, 6b 10 unveiled IC50 values 33.64 8.45 μM, respectively....
Topoisomerase II (TOP-2) is a promising molecular target for cancer therapy. Numerous antibiotics could interact with biologically relevant macromolecules and provoke antitumor potential. Herein, docking studies were used to investigate the binding interactions of 138 against human topoisomerase II-DNA complex. Followed by MD simulations 200 ns MM-GBSA calculations. On other hand, activities most candidates investigated three cell lines using doxorubicin (DOX) as reference drug. Notably,...
Herein, a set of pyridine and pyrimidine derivatives were assessed for their impact on the cell cycle apoptosis. Human breast cancer (MCF7), hepatocellular carcinoma (HEPG2), larynx (HEP2), lung (H460), colon cancers (HCT116 Caco2), hypopharyngeal (FADU), normal Vero lines used. Compounds 8 14 displayed outstanding effects investigated further tested antioxidant activity in MCF7, H460, FADU, HEP2, HEPG2, HCT116, Caco2, cells by measuring superoxide dismutase (SOD), malondialdehyde content...
There is an urgent need to develop therapeutic options for biofilm-producing Staphylococcus aureus (S. aureus). Therefore, the renewed interest in essential oils (EOs), especially carvacrol, linalool and eugenol, has attracted attention of our research group.Multidrug resistance multivirulence profiles addition biofilm production S. strains isolated from cows with mastitis were evaluated using both phenotypic genotypic methods. The antimicrobial antibiofilm activities EOs tested vitro...
Aim: Using molecular hybridization approach, novel 18 quinoline derivatives (6a–11) were designed and synthesized as EGFR-TK inhibitors. Materials & methods: The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) lung (A549) cancer cell lines. Moreover, the most active (6d 8b) further investigated for their potential In addition, cycle analysis apoptosis induction conducted. Results: A considerable cytotoxic attained with IC50 values spanning from 0.06 to 1.12...
The Pharmaceuticals Editorial Office retracts the article "Design and Synthesis of Novel 5-((3-(Trifluoromethyl)piperidin-1-yl)sulfonyl)indoline-2,3-dione Derivatives as Promising Antiviral Agents: In Vitro, Silico, Structure-Activity Relationship Studies" [...].
Donepezil-based rational design of N -substituted quinazoline tethered thioacetamide as potential acetylcholine esterase inhibitors for the treatment Alzheimer's disease.