Document Report Card

ID: ALA1152781

Journal: J Med Chem

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

Authors: Lund BW, Knapp AE, Piu F, Gauthier NK, Begtrup M, Hacksell U, Olsson R.

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.

CiteXplore: 19239230

DOI: 10.1021/jm801532e