A5089714271- Synthesis and biological activity
- Enzyme function and inhibition
- Histone Deacetylase Inhibitors Research
- Synthesis and Catalytic Reactions
- Synthesis and Biological Evaluation
- Protein Degradation and Inhibitors
- Cancer therapeutics and mechanisms
- Synthesis and Characterization of Heterocyclic Compounds
- Chemical Reactions and Mechanisms
- Cholinesterase and Neurodegenerative Diseases
- Click Chemistry and Applications
- Bioactive Compounds and Antitumor Agents
- Cancer Mechanisms and Therapy
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Computational Drug Discovery Methods
- Phenothiazines and Benzothiazines Synthesis and Activities
- Epigenetics and DNA Methylation
- Synthetic Organic Chemistry Methods
- Cancer-related Molecular Pathways
- Synthesis and Reactions of Organic Compounds
- PI3K/AKT/mTOR signaling in cancer
- Peptidase Inhibition and Analysis
- Cytokine Signaling Pathways and Interactions
- HIV/AIDS drug development and treatment
Egyptian Russian University
2016-2025
Martin Luther University Halle-Wittenberg
2021-2024
Leibniz Institute of Plant Biochemistry
2024
Luther University
2024
Logan Hospital
2022
Taif University
2014
On account of their significance as apoptosis inducing agents, merging indole and 3-hydrazinoindolin-2-one scaffolds is a logic tactic for designing pro-apoptotic agents. Consequently, 27 hybrids (6a-r, 9a-f 11a-c) were synthesised evaluated cytotoxicity against MCF-7, HepG-2 HCT-116 cancer cell lines. SAR studies unravelled that N-propylindole derivatives the most active compounds such 6n (MCF-7; IC50=1.04 µM), which displayed significant decrease population in G2/M phase increase early...
In our endeavor towards the development of effective anticancer agents, a novel series pyridine-ureas 8a–n were synthesized. All newly prepared derivatives evaluated in vitro for their growth inhibitory activity proliferation breast cancer MCF-7 cell line. Compounds 8e and 8n found to be most active congeners against cells (IC50 = 0.22 1.88 µM after 48 h treatment; 0.11 0.80 72 treatment, respectively) with increased compared reference drug doxorubicin 1.93 µM). Moreover, eight selected...
Triple-negative breast cancer (TNBC) is a highly aggressive malignancy with limited treatment options due to its heterogeneity and the lack of well-defined molecular targets. In our endeavour towards development novel anti-TNBC agents, herein we report one-pot three-component synthesis spirooxindoles 6a–p, evaluation their potential anti-proliferative activity TNBC MDA-MB-231 cells. Spirooxindoles 6a, 6e 6i emerged as most potent analogues IC50 = 6.70, 6.40 6.70 µM, respectively. Compounds...
Class I histone deacetylases (HDACs) are key regulators of cell proliferation and they frequently dysregulated in cancer cells. We report here the synthesis a novel series class-I selective HDAC inhibitors (HDACi) containing 2-aminobenzamide moiety as zinc-binding group connected with central (piperazin-1-yl)pyrazine or (piperazin-1-yl)pyrimidine moiety. Some compounds were additionally substituted an aromatic capping group. Compounds tested vitro against human HDAC1, 2, 3, 8 enzymes...
Hypoxia in tumors contributes to chemotherapy resistance, worsened by acidosis driven carbonic anhydrases (
In our endeavor towards the development of potent anticancer agents, two different sets biphenylurea-indolinone conjugates, 5a-s and 8a,b were synthesized. The in vitro cytotoxicity synthesized compounds was examined human cancer cell lines, namely MCF-7 breast PC-3 prostate cells using sulforhodamine B (SRB) colorimetric assay. particular, line more susceptible to compounds. Compound 5o (IC50 = 1.04 ± 0.10 μM) emerged as most active member this study against MCF-7, with 7-fold increased...
The vascular endothelial growth factor receptor 2 (VEGFR2) and c-mesenchymal epithelial transition (c-Met) are members of tyrosine kinases which have a crucial role in the process angiogenesis. Isatin moiety is versatile group that shared many compounds targeting both c-Met VEGFR2 kinases. In this study, we designed synthesized different derivatives substituted 3-(triazolo-thiadiazin-3-yl)indolin-2-one (6a-y) as dual inhibitors for enzymes. Eight 6a, 6b, 6e, 6l, 6n, 6r, 6v, 6y were assessed...
Posttranslational modification of proteins by reversible acetylation regulates key biological processes. Histone deacetylases (HDACs) catalyze protein deacetylation and are frequently dysregulated in tumors. This has spurred the development HDAC inhibitors (HDACi). Such epigenetic drugs modulate acetylation, eliminate tumor cells, approved for treatment blood cancers.