Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor ß ligands
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Medicinal Chemistry |
Vol/bind | 52 |
Udgave nummer | 6 |
Sider (fra-til) | 1540-1545 |
ISSN | 0022-2623 |
DOI | |
Status | Udgivet - 2009 |
- Det tidligere Farmaceutiske Fakultet
Forskningsområder
ID: 18652140