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-[1]benzopyrano[3,4-f]quinolines

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-a...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-03, Vol.46 (6), p.1016-1030
Hauptverfasser:	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, Falls, H. Douglass, Lin, Chun W, Nakane, Masake, Miller, Loan, Tyree, Curtis M, Miner, Jeffery N, Jacobson, Peer B, Wilcox, Denise M, Nguyen, Phong, Lane, Benjamin C
Format:	Artikel
Sprache:	eng
Schlagworte:	Allyl Compounds - chemical synthesis Allyl Compounds - chemistry Allyl Compounds - pharmacology Animals Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Binding, Competitive Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Carrageenan Cell Division - drug effects Concanavalin A - pharmacology E-Selectin - genetics E-Selectin - metabolism Edema - chemically induced Edema - drug therapy Humans In Vitro Techniques Ligands Medical sciences NF-kappa B - metabolism Pharmacology. Drug treatments Protein Isoforms Quinolines - chemical synthesis Quinolines - chemistry Quinolines - pharmacology Rats Rats, Sprague-Dawley Receptors, Glucocorticoid - drug effects Receptors, Glucocorticoid - genetics Receptors, Glucocorticoid - metabolism Response Elements Species Specificity Structure-Activity Relationship T-Lymphocytes - cytology T-Lymphocytes - drug effects Transcription Factor AP-1 - metabolism Transcription, Genetic
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