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ID: ALA1147494

Journal: Bioorg Med Chem Lett

Title: Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

Authors: Elmore SW, Pratt JK, Coghlan MJ, Mao Y, Green BE, Anderson DD, Stashko MA, Lin CW, Falls D, Nakane M, Miller L, Tyree CM, Miner JN, Lane B.

Abstract: The SAR at C-5 of the 10-methoxy-2,2,4-trimethylbenzopyrano[3,4-f]quinoline core leading to identification of (-) anti 1-methylcyclohexen-3-yl as the optimum substituent that imparts minimal GR mediated in vitro transcriptional activation while maintaining full transcriptional repression is described. The in vitro profile of these candidates in human cell assays relevant to the therapeutic window of glucocorticoid modulators is outlined.

CiteXplore: 15026058

DOI: 10.1016/j.bmcl.2004.01.044