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Design and Synthesis of Fluorinated RXR Modulators.

D.L. Gernert,R. Ajamie,R.A. Ardecky,M.G. Bell,M.D. Leibowitz,D.A. Mais,C.M. Mapes,P.Y. Michellys,D. Rungta,A. Reifel-Miller,J.S. Tyhonas,N. Yumibe,T.A. Grese

Bioorganic & Medicinal Chemistry Letters（2003）

Cited 27|Views13
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Abstract
Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRα and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the position of fluorination, and improvement in pharmacological profile was demonstrated in some cases.
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rxr modulators
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