Novel selective glucocorticoid receptor agonists (SEGRAs) with a covalent warhead for long-lasting inhibition

Authors :: Oksana Ryabtsova
Hans De Winter
Wim Vanden Berghe
Jurgen Joossens
Koen Augustyns
Pieter Van der Veken
Source :: Bioorganic and medicinal chemistry letters
Publication Year :: 2016
Publisher :: Elsevier BV, 2016.
Abstract: The synthesis and in vitro properties of six analogues of the selective glucocorticoid receptor (GR) agonist GSK866, bearing a warhead for covalent linkage to the glucocorticoid receptor, is described.

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