Literature DB >> 15808489

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

Christopher F Thompson1, Nazia Quraishi, Amjad Ali, James R Tata, Milton L Hammond, James M Balkovec, Monica Einstein, Lan Ge, Georgianna Harris, Theresa M Kelly, Paul Mazur, Shilpa Pandit, Joseph Santoro, Ayesha Sitlani, Chuanlin Wang, Joanne Williamson, Douglas K Miller, Ting-ting D Yamin, Chris M Thompson, Edward A O'Neill, Dennis Zaller, Michael J Forrest, Ester Carballo-Jane, Silvi Luell.   

Abstract

A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

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Year:  2005        PMID: 15808489     DOI: 10.1016/j.bmcl.2005.02.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Minireview: live and let die: molecular effects of glucocorticoids on bone cells.

Authors:  Lorenz C Hofbauer; Martina Rauner
Journal:  Mol Endocrinol       Date:  2009-05-28

Review 2.  Crosstalk in inflammation: the interplay of glucocorticoid receptor-based mechanisms and kinases and phosphatases.

Authors:  Ilse M E Beck; Wim Vanden Berghe; Linda Vermeulen; Keith R Yamamoto; Guy Haegeman; Karolien De Bosscher
Journal:  Endocr Rev       Date:  2009-11-04       Impact factor: 19.871

3.  Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.

Authors:  Jeffrey N Miner; Bob Ardecky; Khalid Benbatoul; Kimberly Griffiths; Christopher J Larson; Dale E Mais; Keith Marschke; Jon Rosen; Eric Vajda; Lin Zhi; Andres Negro-Vilar
Journal:  Proc Natl Acad Sci U S A       Date:  2007-11-21       Impact factor: 11.205

  3 in total

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