| Literature DB >> 19239230 |
Birgitte W Lund1, Anne Eeg Knapp, Fabrice Piu, Natalie K Gauthier, Mikael Begtrup, Uli Hacksell, Roger Olsson.
Abstract
We recently discovered the isoform selective RAR beta 2 ligand 4'-octyl-4-biphenylcarboxylic acid (3, AC-55649). Although 3 is highly potent at RAR beta 2 and displays excellent selectivity, solubility issues make it unsuitable for drug development. Herein we describe the exploration of the SAR in a biphenyl and a phenylthiazole series of analogues of 3. This ultimately led to the design of 28, a novel, orally available ligand with excellent isoform selectivity for the RAR beta 2.Entities:
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Year: 2009 PMID： 19239230 DOI： 10.1021/jm801532e
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446