Future medicinal chemistry · 2024
Design and synthesis of new nicotinamides as immunomodulatory VEGFR-2 inhibitors and apoptosis inducers.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Yousef Reda G, Eissa Ibrahim H, Elkady Hazem, M Mehany Ahmed B, Abo-Saif Mariam Ali, Radwan Mohamed M, ElSohly Mahmoud A, Ibrahim Ibrahim M, Elwan Alaa, El-Zahabi Mohamed Ayman
Аннотация
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 were conducted to evaluate the VEGFR-2 inhibition and cytotoxicity.Results: Compound 16c displayed strongest anti-VEGFR-2 potentiality and good anti-proliferative effects. Compound 16c enhanced apoptosis and caused cell cycle arrest in the Pre-G1 and S phases. Compound 16c boosted the level of the apoptotic caspase-3 and inhibited the level of TNF-α and IL-6 in tumor cells. Molecular docking and molecular dynamics (MD) simulations indicated the outstanding binding potential of compound 16c against VEGFR-2.Conclusion: Compound 16c is a good candidate for the creation of a novel antiangiogenic lead anticancer medication.
Предметные рубрики MeSH
Vascular Endothelial Growth Factor Receptor-2HumansApoptosisDrug DesignNiacinamideMolecular Docking SimulationCell ProliferationProtein Kinase InhibitorsAntineoplastic AgentsStructure-Activity RelationshipMolecular StructureDrug Screening Assays, AntitumorCell Line, TumorMolecular Dynamics SimulationImmunologic Factors