870767-08-1Relevant articles and documents
Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor β ligands
Lund, Birgitte W.,Knapp, Anne Eeg,Piu, Fabrice,Gauthier, Natalie K.,Begtrup, Mikael,Hacksell, Uli,Olsson, Roger
supporting information; experimental part, p. 1540 - 1545 (2009/12/25)
We recently discovered the isoform selective RARβ2 ligand 4′-octyl-4-biphenylcarboxylic acid (3, AC-55649). Although 3 is highly potent at RARβ2 and displays excellent selectivity, solubility issues make it unsuitable for drug development. Herein we descr
COMPOUNDS WITH ACTIVITY AT RETINOIC ACID RECEPTORS
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Page/Page column 43-44, (2008/06/13)
Disclosed herein are novel compounds with activity at RARβ 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
Discovery of a potent, orally available, and isoform-selective retinoic acid β2 receptor agonist
Lund, Birgitte W.,Piu, Fabrice,Gauthier, Natalie K.,Eeg, Anne,Currier, Erika,Sherbukhin, Vladimir,Brann, Mark R.,Hacksell, Uli,Olsson, Roger
, p. 7517 - 7519 (2007/10/03)
4′-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARβ2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorl