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2005
Steroids
U 0300
33- 222
Novel Heterocyclic Glucocorticoids: In vitro Profile and in vivo Efficacy. —
A series of novel ligands for the glucocorticoid receptor containing heterocyclic
substituents at the C-1 position [cf. (IV), (V); 10 examples in all] are prepared and evaluated for a dissociative profile using transrepression and transactivation assays. Compound (IVb) appears to be the most impressive of these new compounds. It is moderately potent, shows efficacy in vivo and is dissociated both in mouse and human cell
lines relative to traditional steroids. — (THOMPSON*, C. F.; et al.; Bioorg. Med.
Chem. Lett. 15 (2005) 8, 2163-2167; Dep. Med. Chem., Merck Res. Lab., Rahway,
NJ 07065, USA; Eng.) — F. Santoso
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