Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.

@article{Lund2009DesignSA,
  title={Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.},
  author={B. W. Lund and A. E. Knapp and F. Piu and N. Gauthier and M. Begtrup and U. Hacksell and R. Olsson},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 6},
  pages={
          1540-5
        }
}
  • B. W. Lund, A. E. Knapp, +4 authors R. Olsson
  • Published 2009
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 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. 
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