| Literature DB >> 17616395 |
Margaret Clackers1, Diane M Coe, Derek A Demaine, George W Hardy, Davina Humphreys, Graham G A Inglis, Michael J Johnston, Haydn T Jones, David House, Richard Loiseau, Doug J Minick, Philip A Skone, Iain Uings, Iain M McLay, Simon J F Macdonald.
Abstract
Starting from an established series of non-steroidal glucocorticoid receptor (GR) agonists, a large array was designed where a metabolically labile benzoxazinone moiety was replaced. Initial hits bound to GR but lacked agonist activity. Following two further iterations, potent GR agonists were discovered with 20D1E1 having NFkappaB agonism pIC(50) 8.8 (103%). Other analogues such as 23D1E1 display a dissociated profile (NFkappaB pIC(50) 8.1 (103%), MMTV pEC(50) 7.02 (36%)). The tetrahydronaphthalene moiety can also be replaced with substituted aryls such as 24E1 and 25E1.Entities:
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Year: 2007 PMID： 17616395 DOI： 10.1016/j.bmcl.2007.06.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823