Title of article
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators
Author/Authors
Steven W Elmore، نويسنده , , John K Pratt، نويسنده , , Michael J. Coghlan، نويسنده , , Yue Mao، نويسنده , , Brian E Green، نويسنده , , David D Anderson، نويسنده , , Michael A. Stashko، نويسنده , , Chun W Lin، نويسنده , , Douglas Falls، نويسنده , , Masaki Nakane، نويسنده , , Loan Miller، نويسنده , , Curtis M Tyree، نويسنده , , Jeffrey N Miner، نويسنده , , Ben Lane، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
7
From page
1721
To page
1727
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794268
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