Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist

…, J Xu, P Zhu, J Gunnet, K Demarest, S Lundeen…

文献索引：Jiang, Weiqin; Fiordeliso, James J.; Allan, George; Linton, Olivia; Tannenbaum, Pamela; Xu, Jun; Zhu, Peifang; Gunnet, Joseph; Demarest, Keith; Lundeen, Scott; Sui, Zhihua Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1471 - 1474

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被引用次数: 13

摘要

Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-diabetic activities. For glucocorticoid receptor (GR) program, we sought an unexplored, synthetically accessible phosphorus-containing steroidal mimetic of mifepristone, suitable for parallel synthesis of analogues. One compound 4a, with high oral bioavailability (59%) in rat, exhibited functional antagonism of GR in oral glucose ...