A5026432056- Synthesis and biological activity
- Angiogenesis and VEGF in Cancer
- Bioactive Compounds and Antitumor Agents
- Synthesis and Biological Evaluation
- Cancer Mechanisms and Therapy
- Quinazolinone synthesis and applications
- PI3K/AKT/mTOR signaling in cancer
- Cancer therapeutics and mechanisms
- Computational Drug Discovery Methods
- HER2/EGFR in Cancer Research
- Synthesis and Reactions of Organic Compounds
- CAR-T cell therapy research
- Chemical Reaction Mechanisms
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer Treatment and Pharmacology
- Cytokine Signaling Pathways and Interactions
- Histone Deacetylase Inhibitors Research
- Plant-based Medicinal Research
- Toxin Mechanisms and Immunotoxins
- Phenothiazines and Benzothiazines Synthesis and Activities
- HIV/AIDS drug development and treatment
- Neuroscience and Neuropharmacology Research
- Biochemical and Molecular Research
- Hepatitis B Virus Studies
Al-Azhar University
2016-2024
Al-Azhar University
2020
A new series of benzoxazole derivatives were designed and synthesised to have the main essential pharmacophoric features VEGFR-2 inhibitors. Cytotoxic activities evaluated for all against two human cancer cell lines, MCF-7 HepG2. Also, effect most cytotoxic on protein concentration was assessed by ELISA. Compounds
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a critical role in cancer angiogenesis. Inhibition of VEGFR-2 activity proved effective suppression tumour propagation. Accordingly, two series new 3-methylquinoxaline derivatives have been designed and synthesised as inhibitors. The were evaluated vitro for their cytotoxic activities against MCF-7and HepG2 cell lines. In addition, the inhibitory target compounds estimated to indicate potential mechanism cytotoxicity. To great...
This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative previous concerned with development VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazole moiety were synthesized and evaluated against three human cancer cell lines, namely, breast (MCF-7), colorectal carcinoma (HCT116), hepatocellular (HepG2). The also kinase activity. biological testing fallouts showed that compound
Among a group of 310 natural antiviral metabolites, our team identified three compounds as the most potent inhibitors against SARS-CoV-2 main protease (PDB ID: 5R84), Mpro. The are sattazolin and caprolactin A B. validated multistage in silico study was conducted using several techniques. First, molecular structures selected metabolites were compared with that GWS, co-crystallized ligand Mpro, structural similarity study. aim this to determine thirty similar (10%) may bind Mpro GWS. Then,...
Herein, a new wave of bis([1, 2, 4]triazolo)[4,3-a:3',4'-c]quinoxaline derivatives have been successfully designed and synthesised. The synthesised were biologically investigated for their cytotoxic activities against HepG2 MCF-7. Also, the tested compounds further examined in vitro VEGFR-2 inhibitory activity. most promising derivative 23j was its apoptotic behaviour cell lines using flow cytometric western-plot analyses. Additional in-silico studies performed to predict how can bind...
There is an urgent need to design new anticancer agents that can prevent cancer cell proliferation even with minimal side effects. Accordingly, two series of 3-methylquinoxalin-2(1H)-one and 3-methylquinoxaline-2-thiol derivatives were designed act as VEGFR-2 inhibitors. The synthesised evaluated in vitro cytotoxic against human lines namely, HepG-2 MCF-7. Also, the assessed for their VEGFR-2inhibitory effect. most promising member 11e further investigated reach a valuable insight about its...
In this study, a set of novel benzoxazole derivatives were designed, synthesised, and biologically evaluated as potential VEGFR-2 inhibitors. Five compounds (12d, 12f, 12i, 12l, 13a) displayed high growth inhibitory activities against HepG2 MCF-7 cell lines further investigated for their activities. The most potent anti-proliferative member 12 l (IC50 = 10.50 μM 15.21 MCF-7, respectively) had the promising activity 97.38 nM). A biological evaluation revealed that compound 12l could arrest...
New nicotinamide derivatives 6, 7, 10, and 11 were designed synthesised based on the essential features of VEGFR-2 inhibitors. Compound 10 revealed highest anti-proliferative activities with IC50 values 15.4 9.8 µM against HCT-116 HepG2, respectively compared to sorafenib (IC50 = 9.30 7.40 µM). 7 owned promising cytotoxic 15.7 15.5 same cell lines, respectively. Subsequently, inhibitory assessed for titled compounds exhibit inhibition sub-micromolar values. Moreover, compound induced cycle...
Background: VEGFR-2 is one of the most effective targets in cancer treatment. Aim: The design and semi-synthesis new theobromine derivatives as potential inhibitors. Methods: In vitro silico evaluation synthesized compounds. Results: Compound 5b demonstrated excellent antiproliferative inhibitory effects with significant apoptotic activity. It modulated immune response by increasing IL-2 reducing TNF-α levels. Docking molecular dynamics simulations revealed compound’s binding affinity...
In this study, a series of seven novel 2,4-dioxothiazolidine derivatives with potential anticancer and VEGFR-2 inhibiting abilities were designed synthesized as inhibitors. The compounds tested in vitro for their to inhibit the growth HepG2 MCF-7 cancer cell lines. Among tested, compound 22 (IC50 = 0.079 μM) demonstrated highest anti-VEGFR-2 efficacy. Furthermore, it significant anti-proliferative activities against 2.04 ± 0.06 1.21 0.04 M). Additionally, also increased total apoptotic rate...
In view of their DNA intercalation activities as anticancer agents, 17 novel [1,2,4]triazolo[4,3-<italic>a</italic>]quinoxaline derivatives have been designed, synthesized and evaluated against HepG2, HCT-116 MCF-7 cells.
In this study, novel VEGFR-2-targeting thiazolidine-2,4-dione derivatives with potential anticancer properties were designed and synthesized. The ability of the to inhibit VEGFR-2 stop growth three different cancer cell types (HT-29, A-549, HCT-116) was examined
Continuing our antecedent work against COVID-19, a set of 5956 compounds traditional Chinese medicine have been virtually screened for their potential SARS-CoV-2 helicase (PDB ID: 5RMM). Initially, fingerprint study with VXG, the ligand target enzyme, disclosed similarity 187 compounds. Then, molecular declared most similar 40 Subsequently, docking studies were carried out to examine binding modes and energies. appropriate 26 subjected in silico ADMET toxicity select convenient inhibitors...
Vascular endothelial cell proliferation and angiogenesis are all crucially impacted by Endothelial Growth Factor Receptor-2 (VEGFR-2). Its expression is significantly boosted throughout pathologic causing the development of tumors. Sothat, inhibition VEGFR-2 has crucial role in cancer treatment. In this study, novel semisynthetic theobromine derivatives were rationally designed as inhibitors subjected to vitro testing for their ability block activation. Furthermore, antiproliferative effects...
VEGFR-2, the subtype receptor tyrosine kinase (RTK) responsible for angiogenesis, is expressed in various cancer cells. Thus, VEGFER-2 inhibition an efficient approach discovery of new anticancer agents. Accordingly, a set nicotinamide derivatives were designed and synthesized to be VEGFR-2 inhibitors. The chemical structures confirmed using IR, 1H-NMR, 13C-NMR spectroscopy. obtained compounds examined their anti-proliferative activities against human cell lines (HCT-116 HepG2). inhibitory...
Abstract In this work novel 2,4‐dioxothiazolidine‐derived compounds targeting VEGFR‐2 were designed and synthesized. Such evaluated for their anti‐proliferative inhibitory abilities. Compound 17 specifically demonstrated the strongest activity against HCT‐116 cell line, with an IC 50 value of 10.09 μM. Additionally, 15 , 18 19 revealed good effects values 12.46, 16.87, 12.35 μM, respectively. potent anti‐VEGFR‐2 efficacy, 0.068 which was comparable to sorafenib (IC 0.058 μM). induced...