2. Academic Validation
  3. Design and synthesis of fluorinated RXR modulators

Design and synthesis of fluorinated RXR modulators

  • Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5. doi: 10.1016/s0960-894x(03)00703-0.
D L Gernert 1,  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
Affiliations

Affiliation

  • 1 Discovery Chemistry Research, Lilly Research Laboratories, Indianapolis, IN, USA. dgernert@lilly.com
PMID: 12951091 DOI: 10.1016/s0960-894x(03)00703-0
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.

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