Title of article
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity
Author/Authors
Cameron J. Smith، نويسنده , , Amjad Ali، نويسنده , , James M. Balkovec، نويسنده , , Donald W. Graham، نويسنده , , Milton L. Hammond، نويسنده , , Gool F. Patel، نويسنده , , Gregory P. Rouen، نويسنده , , Scott K. Smith، نويسنده , , James R. Tata، نويسنده , , Monica Einstein، نويسنده , , Lan Ge، نويسنده , , Georgianna S. Harris، نويسنده , , Theresa M. Kelly، نويسنده , , Paul Mazur، نويسنده , , Chris M. Thompson، نويسنده , , Chuanlin F. Wang، نويسنده , , Joanne M. Williamson، نويسنده , , Douglas K. Miller، نويسنده , , Shilpa Pandit، نويسنده , , Joseph C. Santoro، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
2926
To page
2931
Abstract
A novel series of selective ligands for the human glucocorticoid receptor is described. Structure–activity studies focused on variation of B-ring size, ketal ring size, and ketal substitution. These analogs were found to be potent and selective ligands for GR and have partial agonist profiles in functional assays for transactivation (TAT, GS) and transrepression (IL-6). Of these compounds, 27, 28, and 35 were evaluated further in a mouse LPS-induced TNF-α secretion model. Compound 28 had an ED50 of 14.1 mg/kg compared with 0.5 mg/kg for prednisolone in the same assay.
Keywords
Glucocorticoid , Dissociation , Transrepression , inflammation , transactivation
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795701
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