2. Academic Validation
  3. Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

  • Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7. doi: 10.1016/j.bmcl.2005.02.009.
Christopher F Thompson 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christopher_thompson@merck.com
PMID: 15808489 DOI: 10.1016/j.bmcl.2005.02.009
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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