Alaa Elwan
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View article: Design, synthesis, and cytotoxic evaluation of quinazoline-based derivatives as VEGER-2 inhibitors: comparative study against EGFR kinase activity, induction of apoptosis, and molecular docking study
Design, synthesis, and cytotoxic evaluation of quinazoline-based derivatives as VEGER-2 inhibitors: comparative study against EGFR kinase activity, induction of apoptosis, and molecular docking study Open
A novel series of quinazoline-based compounds were designed and synthesized as modified analogues to certain known VEGFR-2 inhibitors, as an extension of our work on the design and synthesis of new VEGFR-2 inhibitors.
View article: Modification of Quinazoline-Based Derivatives as Veger-2 Inhibitors and Apoptosis Inducer: Design, Synthesis, Molecular Docking, and Anti-Proliferative Evaluation
Modification of Quinazoline-Based Derivatives as Veger-2 Inhibitors and Apoptosis Inducer: Design, Synthesis, Molecular Docking, and Anti-Proliferative Evaluation Open
View article: Targeting VEGFR-2 in breast cancer: synthesis and <i>in silico</i> and <i>in vitro</i> characterization of quinoxaline-based inhibitors
Targeting VEGFR-2 in breast cancer: synthesis and <i>in silico</i> and <i>in vitro</i> characterization of quinoxaline-based inhibitors Open
Design, synthesis and in vitro and in silico studies of novel quinoxaline-based derivatives as antitumor VEGFR-2 inhibitors with apoptotic activities.
View article: Design and synthesis of new nicotinamides as immunomodulatory VEGFR-2 inhibitors and apoptosis inducers
Design and synthesis of new nicotinamides as immunomodulatory VEGFR-2 inhibitors and apoptosis inducers Open
Background: Nicotinamide-based VEGFR-2 inhibitors have good contribution in drug discovery. Aim: Development of novel nicotinamides as VEGFR-2 inhibitors. Methods: different in vitro and in silico assays …
View article: Discovery of new thiazolidine-2,4-dione derivatives as potential VEGFR-2 inhibitors: In vitro and in silico studies
Discovery of new thiazolidine-2,4-dione derivatives as potential VEGFR-2 inhibitors: In vitro and in silico studies Open
View article: New nicotinamide derivatives as potential anticancer agents targeting VEGFR-2: design, synthesis, <i>in vitro</i> , and <i>in silico</i> studies
New nicotinamide derivatives as potential anticancer agents targeting VEGFR-2: design, synthesis, <i>in vitro</i> , and <i>in silico</i> studies Open
Herin, new nicotinamide candidates were designed and synthesized as VEGFR-2 inhibitors. In vitro antiproliferative activities were assessed against MCF-7, HepG-2 and HCT-116 cancer cell lines. The top cytotoxic members 15a, <…
View article: PYRIDINE DERIVATIVES AS ANTICANCER AGENTS: FDA-APPROVED DRUGS AND PROMISING REPORTED COMPOUNDS
PYRIDINE DERIVATIVES AS ANTICANCER AGENTS: FDA-APPROVED DRUGS AND PROMISING REPORTED COMPOUNDS Open
Pyridine derivatives are a family of heterocyclic nitrogenous compounds possessing many of applications in the discovery of anticancer drug. This synthetic category serve as the potent class of compounds in the treatment of many types of t…
View article: VEGFER-2 INHIBITORS AND QUINAZOLINE-BASED ANTICANCER AGENTS
VEGFER-2 INHIBITORS AND QUINAZOLINE-BASED ANTICANCER AGENTS Open
Inhibitors of vascular endothelial growth factor receptor -2 (VEGFR-2) are crucial biological targets for the development of novel anticancer medications. Quinazoline also plays an important role as one of the building elements of numerous…
View article: Synthesis, biological evaluation and computer-aided discovery of new thiazolidine-2,4-dione derivatives as potential antitumor VEGFR-2 inhibitors
Synthesis, biological evaluation and computer-aided discovery of new thiazolidine-2,4-dione derivatives as potential antitumor VEGFR-2 inhibitors Open
Design, synthesis, in vitro and in silico studies of novel thiazolidine-2,4-diones as antitumor VEGFR-2 inhibitors with apoptotic activities.
View article: Structure-Based Virtual Screening, Docking, ADMET, Molecular Dynamics, and MM-PBSA Calculations for the Discovery of Potential Natural SARS-CoV-2 Helicase Inhibitors from the Traditional Chinese Medicine
Structure-Based Virtual Screening, Docking, ADMET, Molecular Dynamics, and MM-PBSA Calculations for the Discovery of Potential Natural SARS-CoV-2 Helicase Inhibitors from the Traditional Chinese Medicine Open
Continuing our antecedent work against COVID-19, a set of 5956 compounds of traditional Chinese medicine have been virtually screened for their potential against SARS-CoV-2 helicase (PDB ID: 5RMM). Initially, a fingerprint study with VXG, …
View article: Anti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: <i>in vitro</i> and <i>in silico</i> studies
Anti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: <i>in vitro</i> and <i>in silico</i> studies Open
New nicotinamide derivatives 6, 7, 10, and 11 were designed and synthesised based on the essential features of the VEGFR-2 inhibitors. Compound 10 revealed the highest anti-proliferative activities with I…
View article: Modified Benzoxazole-Based VEGFR-2 Inhibitors and Apoptosis Inducers: Design, Synthesis, and Anti-Proliferative Evaluation
Modified Benzoxazole-Based VEGFR-2 Inhibitors and Apoptosis Inducers: Design, Synthesis, and Anti-Proliferative Evaluation Open
This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative of our previous work concerned with the development of VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazol…
View article: A Multistage In Silico Study of Natural Potential Inhibitors Targeting SARS-CoV-2 Main Protease
A Multistage In Silico Study of Natural Potential Inhibitors Targeting SARS-CoV-2 Main Protease Open
Among a group of 310 natural antiviral natural metabolites, our team identified three compounds as the most potent natural inhibitors against the SARS-CoV-2 main protease (PDB ID: 5R84), Mpro. The identified compounds are sattazolin and ca…
View article: Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, <i>in silico</i> studies, and antiproliferative evaluation
Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, <i>in silico</i> studies, and antiproliferative evaluation Open
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, and 13a) displayed high gr…
View article: Design, Synthesis, In Silico and In Vitro Studies of New Immunomodulatory Anticancer Nicotinamide Derivatives Targeting VEGFR-2
Design, Synthesis, In Silico and In Vitro Studies of New Immunomodulatory Anticancer Nicotinamide Derivatives Targeting VEGFR-2 Open
VEGFR-2, the subtype receptor tyrosine kinase (RTK) responsible for angiogenesis, is expressed in various cancer cells. Thus, VEGFER-2 inhibition is an efficient approach for the discovery of new anticancer agents. Accordingly, a new set o…
View article: Design, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugates <i>via</i> a 2-Thioacetamido linker as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers
Design, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugates <i>via</i> a 2-Thioacetamido linker as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers Open
A novel series of 2-thioacetamide linked benzoxazole-benzamide conjugates 1–15 was designed as potential inhibitors of the vascular endothelial growth factor receptor-2 (VEGFR-2). The prepared compounds were evaluated for the…
View article: Triazoloquinoxalines-based DNA intercalators-Topo II inhibitors: design, synthesis, docking, ADMET and anti-proliferative evaluations
Triazoloquinoxalines-based DNA intercalators-Topo II inhibitors: design, synthesis, docking, ADMET and anti-proliferative evaluations Open
Sixteen [1, 2, 4]triazolo[4,3-a]quinoxalines as DNA intercalators-Topo II inhibitors have been prepared and their anticancer actions evaluated towards three cancer cell lines. The new compounds affected on high percentage of MCF-7. Derivat…
View article: New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and <i>in silico</i> studies
New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and <i>in silico</i> studies Open
A new series of benzoxazole derivatives were designed and synthesised to have the main essential pharmacophoric features of VEGFR-2 inhibitors. Cytotoxic activities were evaluated for all derivatives against two human cancer cell lines, MC…
View article: Discovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-<i>a</i>:3',4'-<i>c</i>]quinoxaline derivatives as anticancer agents and apoptosis inducers
Discovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-<i>a</i>:3',4'-<i>c</i>]quinoxaline derivatives as anticancer agents and apoptosis inducers Open
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 derivatives were biologically investigated for their cytotoxic activities aga…
View article: Discovery of new 3-methylquinoxalines as potential anti-cancer agents and apoptosis inducers targeting VEGFR-2: design, synthesis, and <i>in silico</i> studies
Discovery of new 3-methylquinoxalines as potential anti-cancer agents and apoptosis inducers targeting VEGFR-2: design, synthesis, and <i>in silico</i> studies Open
There is an urgent need to design new anticancer agents that can prevent cancer cell proliferation even with minimal side effects. Accordingly, two new series of 3-methylquinoxalin-2(1H)-one and 3-methylquinoxaline-2-thiol derivativ…
View article: Design, synthesis, docking, ADMET studies, and anticancer evaluation of new 3-methylquinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers
Design, synthesis, docking, ADMET studies, and anticancer evaluation of new 3-methylquinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers Open
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a critical role in cancer angiogenesis. Inhibition of VEGFR-2 activity proved effective suppression of tumour propagation. Accordingly, two series of new 3-methylquinoxaline der…