72136-99-3Relevant articles and documents
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist
Jiang, Weiqin,Fiordeliso, James J.,Allan, George,Linton, Olivia,Tannenbaum, Pamela,Xu, Jun,Zhu, Peifang,Gunnet, Joseph,Demarest, Keith,Lundeen, Scott,Sui, Zhihua
, p. 1471 - 1474 (2007)
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 tolerance test (OGTT). Thus this series of compounds might be potentially useful for the treatment of type II diabetes.