Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists

  • J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t.
John Regan  1 ,  Thomas W Lee ,  Renée M Zindell ,  Younes Bekkali ,  Jörg Bentzien ,  Thomas Gilmore ,  Abdelhakim Hammach ,  Thomas M Kirrane ,  Alison J Kukulka ,  Daniel Kuzmich ,  Richard M Nelson ,  John R Proudfoot ,  Mark Ralph ,  Josephine Pelletier ,  Donald Souza ,  Lijiljana Zuvela-Jelaska ,  Gerald Nabozny ,  David S Thomson
Affiliations
  • 1. Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA. [email protected]
PMID: 17181172 DOI: 10.1021/jm061273t
Abstract

We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.