%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