2. Academic Validation
  3. Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators

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

  • Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7. doi: 10.1016/j.bmcl.2004.01.044.
Steven W Elmore 1,  John K Pratt,  Michael J Coghlan,  Yue Mao,  Brian E Green,  David D Anderson,  Michael A Stashko,  Chun W Lin,  Douglas Falls,  Masaki Nakane,  Loan Miller,  Curtis M Tyree,  Jeffrey N Miner,  Ben Lane
Affiliations

Affiliation

  • 1 Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. steve.elmore@abbott.com
PMID: 15026058 DOI: 10.1016/j.bmcl.2004.01.044
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.

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