Heterocycles · 2006 · 11 citations · 32 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructure-activity RelationshipsLigand-based DesignPotency OptimizationVitamin ChemistryVitamin DVitamin D DisordersVitamin D MetabolismAntagonistic InteractionsBiological Evaluation ReportBiomolecular Binding AffinityPhenyl Ring ReplacementVitamin AnaloguesVitamin D AnalogsVitamin D AnaloguesVitamin D Receptors
Novel vitamin D receptor (VDR) antagonists, 1α-hydroxy-24-phenylvitamin D 3 -26,23-lactones were synthesized by Trost's methodology.The biological evaluation revealed that both the binding affinity for VDR and antagonistic activity were affected by the orientation of the phenyl group on the lactone ring.The modification of the 2α-position of the 24-phenylvitamin D 3 lactones improved the antagonistic activity up to 41 times higher than that of TEI-9647.
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Steven Collins, Francis W. Ruscetti, Robert E. Gallagher et al. · The Journal of Experimental Medicine · 1979 · 595 citations · Full text