Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators

…, M Emery, M Grynfarb, A Goos-Nilsson

Index: Link; Sorensen, Bryan K.; Patel, Jyoti; Arendsen, David; Li, Gaoquan; Swanson, Susan; Nguyen, Bach; Emery, Maurice; Grynfarb, Marlena; Goos-Nilsson, Annika Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4169 - 4172

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Citation Number: 9

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered typified by the subnanomolar acid 12 (GR binding IC 50 = 0.6 nM). ... The synthesis and biochemical profile of the potent ...

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