A5057264898- Synthesis and biological activity
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Sirtuins and Resveratrol in Medicine
- Chronic Myeloid Leukemia Treatments
- Quinazolinone synthesis and applications
- Histone Deacetylase Inhibitors Research
- Synthesis and Characterization of Heterocyclic Compounds
- Calcium signaling and nucleotide metabolism
- Fungal Plant Pathogen Control
- Synthesis and Biological Evaluation
- Multicomponent Synthesis of Heterocycles
- Acute Myeloid Leukemia Research
- Phytochemicals and Antioxidant Activities
- HIV/AIDS drug development and treatment
- Essential Oils and Antimicrobial Activity
- interferon and immune responses
- Metabolism, Diabetes, and Cancer
- Biochemical effects in animals
- Retinoids in leukemia and cellular processes
- Phytochemical compounds biological activities
- Cholinesterase and Neurodegenerative Diseases
- Phytochemistry and Biological Activities
- Advanced Breast Cancer Therapies
- Drug Solubulity and Delivery Systems
Minia University
2013-2025
West Suburban Medical Center
2025
Kumamoto University
2015-2024
Cornell University
2024
King Fahd Medical City
2021
National Research Centre
2021
University of Illinois Chicago
2021
The University of Texas MD Anderson Cancer Center
2018
The University of Texas Health Science Center at Houston
2017
University of the Sciences
2015
The structure-based design introduced indoles as an essential motif in designing new selective estrogen receptor modulators employed for treating breast cancer. Therefore, here, a series of synthesized vanillin-substituted indolin-2-ones were screened against the NCI-60 cancer cell panel followed by vivo, vitro, and silico studies. Physicochemical parameters evaluated with HPLC SwissADME tools. compounds demonstrated promising anti-cancer activity MCF-7 line (GI = 6-63%). compound highest...
We developed and synthesized tetrahydropyrimidine derivatives as possible cytotoxic agents to inhibit EGFR VEGFR-2 in the present study. Our study completely assesses efficiency of pyrimidine-based
In an attempt to develop potent antitumor agents, new 1,3,4-thiadiazole derivatives were synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines, including the K562 chronic myelogenous leukemia line that expresses Bcr-Abl tyrosine kinase. N-(5-Nitrothiazol-2-yl)-2-((5-((4-(trifluoromethyl)phenyl)amino)-1,3,4-thiadiazol-2-yl)thio)acetamide (2) inhibited Abl protein kinase with IC50 value of 7.4 µM showed selective activity against positive line. Furthermore,...
Abstract Sirtuin 2 (SIRT2) is a member of the sirtuin protein family, which includes lysine deacylases that are NAD + -dependent and organize several biological processes. Different forms cancer have been associated with dysregulation SIRT2 activity. Hence, identifying potent inhibitors for has piqued considerable attention in drug discovery community. In current study, Natural Products Atlas (NPAtlas) database was mined to hunt potential utilizing silico techniques. Initially, performance...
With advances in refractive surgery and demand for cataract removal lens replacement, the ocular use of nonsteroidal anti‐inflammatory drugs (NSAIDs) has increased. One most commonly used NSAIDs is diclofenac (Diclo). In this study, cyclodextrins (CDs), α ‐, β γ HP‐ ‐CDs, were investigated with vitro irritation vivo ulceration models rabbits to reduce Diclo toxicity. Diclo‐, ‐CD inclusion complexes prepared characterized Diclo‐CD evaluated corneal permeation, red blood cell (RBCs)...
Epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) are crucial targetable enzymes in cancer management. Therefore, herein, new 2-[(5-((1H-indol-3-yl)methyl)-1,3,4-oxadiazol-2-yl)thio]-N-(thiazol/benzothiazol-2-yl)acetamides (2a–i) were designed synthesized as EGFR COX-2 inhibitors. The cytotoxic effects of compounds 2a–i on HCT116 human colorectal carcinoma, A549 lung adenocarcinoma, A375 melanoma cell lines determined using MTT assay....
A novel series of dihydropyrimidine/sulphonamide hybrids 3a–j with anti-inflammatory properties have been developed and tested as dual mPGES-1/5-LOX inhibitors. In vitro assay, results showed that compounds 3c , 3e 3h 3j were the most effective inhibitors mPGES-1 5-LOX activities. Compound was potent inhibitor IC 50 values 0.92 µM 1.98 µM, respectively. vivo, studies demonstrated 3h, had considerable activity, EI% ranging from 29% to 71%. Compounds equivalent celecoxib after first hour but...
The discovery of the chimeric tyrosine kinase breakpoint cluster region kinase-Abelson (BCR-ABL)-targeted drug imatinib conceptually changed treatment chronic myelogenous leukemia (CML). However, some CML patients show resistance to imatinib. To address this issue, artificial heterocyclic compounds have been identified as BCR-ABL inhibitors. Here we examined whether plant-derived pentacyclic triterpenoid gypsogenin and/or their derivatives inhibitory activity against BCR-ABL. Among three...
Soft corals have been endorsed as a plentiful source of bioactive compounds with promising anti-inflammatory activities; therefore, exploring their potential metabolites has stimulated growing research interest.To investigate the soft coral, Nephthea sp., in its bulk and silver nanostructure. Metabolomics analysis followed by molecular docking studies, was also conducted order to explore predict secondary that might provide inhibitory actions on inflammation.The petroleum ether ethyl acetate...
Rehabilitation needs are increasing globally due to population growth, aging population, high survival rates for people with disability, and severe health conditions. In the past few years, new telecommunication-based practices, including various forms of e-rehabilitation have gained attention all over world, Kingdom Saudi Arabia (KSA). Telerehabilitation is an alternative way delivering rehabilitation services in which information communication technologies used expedite between care...
Imatinib, an Abelson (ABL) tyrosine kinase inhibitor, is a lead molecular-targeted drug against chronic myelogenous leukemia (CML). To overcome its resistance and adverse effects, new inhibitors of ABL are needed. Our previous study showed that the benzyl ester gypsogenin (1c), pentacyclic triterpene, has anti-ABL subsequent anti-CML activity. optimize activities, esters carefully selected triterpenes (PT1-PT6), from different classes comprising oleanane, ursane lupane, substituted (GP1-GP5)...
FMS-like tyrosine kinase 3 (FLT3) mutations occur in approximately 30% of acute myeloid leukemia (AML) patients. In the current study, oxindole chemotype is employed as a structural motif for design new FLT3 inhibitors potential hits AML irradiation. Cell-based screening was performed with 18 derivatives and 5a-c inhibited 68%-73% 83%-91% internal tandem duplication (ITD)-mutated MV4-11 cell growth 48- 72-h treatments while only 0%-2% 27%-39% wild-type THP-1 cells. The most potent compound...
Abstract New 3-substituted oxindole derivatives were designed and synthesized as antiproliferative agents. The activity of compounds 6a–j was evaluated against 60 NCI cell lines. Among these tested compounds, 6f 6g showed remarkable activity, specifically leukemia breast cancer Compound the most promising agent MCF-7 (human cancer) with an IC 50 value 14.77 µM compared to 5-fluorouracil (5FU) (IC = 2.02 µM). Notably, compound hampered receptor tyrosine EGFR fundamentally 1.38 µM, reference...
S-trityl-l-cysteine (STLC) is a well-recognized lead compound known for its anticancer activity owing to potent inhibitory effect on human mitotic kinesin Eg5. STLC contains two free terminal amino and carboxyl groups that play pivotal roles in binding the Eg5 pocket. On other hand, such zwitterion structure complicates clinical development of because solubility issues. Masking either these radicals reduces or abolishes against We recently identified characterized new class nicotinamide...
Protein kinases regulate cellular activities and make up over 60% of oncoproteins proto-oncoproteins. Among these kinases, FLT3 is a member class III receptor tyrosine kinase family which abundantly expressed in individuals with acute leukemia. Our previous oxindole-based hit has particular affinity toward (IC
Abstract Background Solid organ transplant (SOT) recipients are vulnerable to infections with multi-drug resistant organisms. Studies have shown that SOT patients often do not receive adequate empiric antimicrobials for serious Gram-negative infections. Knowledge of epidemiologic differences in resistance rates this population may help guide antibiotic choices patients. Cohort A Methods We performed a retrospective cohort study comparing susceptibility sepsis (cohort A) between 1/1/2021 and...
Tubulin polymerization inhibitors have emerged as interesting anticancer therapies. We present the design, synthesis, and structural elucidation of novel thiazole-based derivatives to identify tubulin with potent antiproliferative efficacy strong inhibition polymerization. The compounds consist two scaffolds. Scaffold A 10a-e scaffold B 13a-e. structures newly synthesized 13a-e were validated using 1H NMR, 13C elemental analysis. most effective antitubulin derivative was 10a, exhibiting an...
Abstract Despite various inhibitors targeting the zinc center(s) of enzymes, drugs that target fingers have not been examined in detail. We previously developed a dithiol compound named SN‐1 has an inhibitory effect on function finger transcription factors, but its mechanism action yet elucidated. To establish general principle for new drugs, details against protein were examined. As zinc‐finger‐containing protein, we focused TRAF6, which is related to cancer and inflammation. Binding TRAF6...