Search results for "Sphingosine Kinase 2"

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Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity.

2019

The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7‐bromo‐2‐(2‐phenylethyl)‐2,3,4,5‐tetrahydro‐1,4‐epoxynaphtho[1,2‐b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti‐inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil–endothelial cell interactions. The information obtained from our theoretical and experimental study can be us…

medicine.drug_classCell SurvivalNeutrophilsFísico-Química Ciencia de los Polímeros ElectroquímicaCellAnti-Inflammatory AgentsPharmaceutical ScienceSYNTHESIS01 natural sciencesPeripheral blood mononuclear cellAnti-inflammatoryANTI-INFLAMMATORY ACTIVITYchemistry.chemical_compoundStructure-Activity RelationshipDrug DiscoverymedicineCell AdhesionHuman Umbilical Vein Endothelial CellsCytotoxic T cellHumansMOLECULAR MODELINGAzepineEnzyme Inhibitors010405 organic chemistryBIOASSAYSCiencias QuímicasSphingosine Kinase 2AdhesionAzepines0104 chemical sciencesMolecular Docking Simulation010404 medicinal & biomolecular chemistrySPHK2Phosphotransferases (Alcohol Group Acceptor)medicine.anatomical_structurechemistrySPHINGOSINE KINASE 2 INHIBITORSDrug DesignCancer researchEpoxy CompoundsEndothelium VascularCIENCIAS NATURALES Y EXACTASProtein BindingArchiv der Pharmazie
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