%0 Journal Article %A Lund, Birgitte W. %A Knapp, Anne Eeg %A Piu, Fabrice %A Gauthier, Natalie K. %A Begtrup, Mikael %A Hacksell, Uli %A Olsson, Roger %D 2009 %T Design, Synthesis, and Structure−Activity Analysis of Isoform-Selective Retinoic Acid Receptor β Ligands %U https://acs.figshare.com/articles/journal_contribution/Design_Synthesis_and_Structure_Activity_Analysis_of_Isoform_Selective_Retinoic_Acid_Receptor_Ligands/2868631 %R 10.1021/jm801532e.s002 %2 https://acs.figshare.com/ndownloader/files/4566475 %K solubility issues %K phenylthiazole series %K Receptor β LigandsWe %K AC %K RAR β2 %K SAR %K isoform selectivity %K ligand %K drug development %X 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 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 RARβ2. %I ACS Publications