Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2, 5-dihydro-2, 2, 4-trimethyl-1H …

…, ME Kort, MJ Coghlan, JL Moore, R Tang…

文献索引：Kym, Philip R.; Kort, Michael E.; Coghlan, Michael J.; Moore, Jimmie L.; Tang, Rui; Ratajczyk, James D.; Larson, Daniel P.; Elmore, Steven W.; Pratt, John K.; Stashko, Michael A.; Douglass Falls; Lin, Chun W.; Nakane, Masake; Miller, Loan; Tyree, Curtis M.; Miner, Jeffery N.; Jacobson, Peer B.; Wilcox, Denise M.; Nguyen, Phong; Lane, Benjamin C. Journal of Medicinal Chemistry, 2003 , vol. 46, # 6 p. 1016 - 1030

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被引用次数: 96

摘要

The preparation and characterization of a series of C-10 substituted 5-allyl-2, 5-dihydro-2, 2, 4-trimethyl-1H-[1] benzopyrano [3, 4-f] quinolines as a novel class of selective ligands for the glucocorticoid receptor is described. Substitution at the C-10 position of the tetracyclic core with linear, two-atom appendages (OCH3, OCF2H, NHMe, SMe, CH CH2, C⋮ CH, CH2OH) provided molecules of high affinity (K i= 2-8 nM) for the human glucocorticoid receptor ( ...