Novel selective glucocorticoid receptor agonists (SEGRAs) with a covalent warhead for long-lasting inhibition. Issue 20 (15th October 2016)

• Record Type: Journal Article
• Authors: Ryabtsova, Oksana; Joossens, Jurgen; Van Der Veken, Pieter; Vanden Berghe, Wim; Augustyns, Koen; De Winter, Hans
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 20(2016)
• Page Start: 5032
• Page End: 5038
• Publication Date: 2016-10-15
• Subjects: Covalent inhibition -- Glucocorticoid receptor -- Segra -- GSK866 -- Inflammation; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.08.091
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: The synthesis of novel SEGRA analogues with warhead for covalent binding is described. Reversible inhibition could be observed. Irreversible inhibition was not observed. 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.