Journal of Medicinal Chemistry · 2019 · 70 citations · 12 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructure-activity RelationshipsEnzyme InhibitionLigand-based DesignOncology PharmacologyStructure-activity Relationship AnalysisCopper-dependent Enzyme FunctionHalf-maximal Inhibitory ConcentrationHigh-throughput Screening AssaysInhibitor ScreeningLysyl Oxidase Cross-linkingLysyl Oxidase InhibitionMedicinal Chemistry ApplicationsStructure - Activity Relationship Optimization
) in a LOX enzyme activity assay. Further SAR optimization yielded the orally bioavailable LOX inhibitor CCT365623 with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.
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