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Imidazo[2,1-b]benzothiazol Derivatives as Potential Allosteric Inhibitors of the Glucocorticoid Receptor. 2018
Michael S Christodoulou, and
Federico Dapiaggi, and
Francesca Ghiringhelli, and
Stefano Pieraccini, and
Maurizio Sironi, and
Marianna Lucafò, and
Debora Curci, and
Giuliana Decorti, and
Gabriele Stocco, and
Chandra Sekhar Chirumamilla, and
Wim Vanden Berghe, and
Patrick Balaguer, and
Benoît Y Michel, and
Alain Burger, and
Egle M Beccalli, and
Daniele Passarella, and
Nadine Martinet
DISFARM, Sezione di Chimica Generale e Organica "A. Marchesini", Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.
Glucocorticoid receptor (GCR) transactivation reporter gene assays were used as an initial high-throughput screening on a diversified library of 1200 compounds for their evaluation as GCR antagonists. A class of imidazo[2,1-b]benzothiazole and imidazo[2,1-b]benzoimidazole derivatives were identified for their ability to modulate GCR transactivation and anti-inflammatory transrepression effects utilizing GCR and NF-κB specific reporter gene assays. Modeling studies on the crystallographic structure of the GCR ligand binding domain provided three new analogues bearing the tetrahydroimidazo[2,1-b]benzothiazole scaffold able to antagonize the GCR in the presence of dexamethasone (DEX) and also defined their putative binding into the GCR structure. Both mRNA level measures of GCR itself and its target gene GILZ, on cells treated with the new analogues, showed a GCR transactivation inhibition, thus suggesting a potential allosteric inhibition of the GCR.
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