Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor ß ligands
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Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor ß ligands. / Lund, Birgitte W.; Knapp, Anne Eeg; Piu, Fabrice; Gauthier, Natalie K; Begtrup, Mikael; Hacksell, Uli; Olsson, Roger.
I: Journal of Medicinal Chemistry, Bind 52, Nr. 6, 2009, s. 1540-1545.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor ß ligands
AU - Lund, Birgitte W.
AU - Knapp, Anne Eeg
AU - Piu, Fabrice
AU - Gauthier, Natalie K
AU - Begtrup, Mikael
AU - Hacksell, Uli
AU - Olsson, Roger
N1 - Keywords: Cell Line, Tumor; Drug Design; Humans; Ligands; Receptors, Retinoic Acid; Structure-Activity Relationship
PY - 2009
Y1 - 2009
N2 - 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.
AB - 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.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1021/jm801532e
DO - 10.1021/jm801532e
M3 - Journal article
C2 - 19239230
VL - 52
SP - 1540
EP - 1545
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 6
ER -
ID: 18652140