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• W2023595238 startingPage "2879" @default.
• W2023595238 abstract "A novel class of functional ligands for the human glucocorticoid receptor is described. Substituents in the C-10 position of the tetracyclic core are essential for glucocorticoid receptor (GR) selectivity versus other steroid receptors. The C-5 position is derivatized with meta-substituted aromatic groups, resulting in analogues with a high affinity for GR (K(i) = 2.4-9.3 nM) and functional activity comparable to prednisolone in reporter gene assays of glucocorticoid-mediated gene transcription. The biological activity of these novel quinolines was also prednisolone-equivalent in whole cell assays of glucocorticoid function, and compound 13 was similar to prednisolone (po ED(50) = 2.8 mpk for 13 vs ED(50) = 1.2 mpk for prednisolone) in a rodent model of asthma (sephadex-induced eosinophil influx)." @default.
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• W2023595238 date "2001-08-01" @default.
• W2023595238 modified "2023-10-18" @default.
• W2023595238 title "Synthesis and Characterization of Non-Steroidal Ligands for the Glucocorticoid Receptor: Selective Quinoline Derivatives with Prednisolone-Equivalent Functional Activity" @default.
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• W2023595238 doi "https://doi.org/10.1021/jm010228c" @default.
• W2023595238 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11520196" @default.
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