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Basic Information

ID: ALA1136229

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of fluorinated RXR modulators.

Authors: Gernert DL, Ajamie R, Ardecky RA, Bell MG, Leibowitz MD, Mais DA, Mapes CM, Michellys PY, Rungta D, Reifel-Miller A, Tyhonas JS, Yumibe N, Grese TA.

Abstract: Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha 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.

CiteXplore: 12951091

DOI: 10.1016/s0960-894x(03)00703-0