Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor ß ligands
Research output: Contribution to journal › Journal article › Research › peer-review
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.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 52 |
Issue number | 6 |
Pages (from-to) | 1540-1545 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 2009 |
Bibliographical note
Keywords: Cell Line, Tumor; Drug Design; Humans; Ligands; Receptors, Retinoic Acid; Structure-Activity Relationship
- Former Faculty of Pharmaceutical Sciences
Research areas
ID: 18652140