Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

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Michellys PY, Boehm MF, Chen JH, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Yumibe N, Ardecky RJ

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4071-5.

PubMed ID

14592510 [ View in PubMed

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Abstract

New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their metabolic properties (exposure in IRC male mice) and show a dramatic increase of exposure compared to our reference compound, 3 (LG101506).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
LG-100268	Retinoic acid receptor RXR-beta	Ki (nM)	75	N/A	N/A	Details