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Design and synthesis of fluorinated RXR modulators.

D L Gernert1, R Ajamie, R A Ardecky

  • 1Discovery Chemistry Research, Lilly Research Laboratories, Indianapolis, IN, USA. dgernert@lilly.com

Bioorganic & Medicinal Chemistry Letters
|September 3, 2003
PubMed
Summary
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New fluorinated trienoic acids were synthesized and tested. Their ability to bind and activate RXR (Retinoid X Receptor) depended on fluorination position, showing improved profiles in some cases.

Area of Science:

  • Medicinal Chemistry
  • Molecular Pharmacology
  • Drug Discovery

Background:

  • Retinoid X Receptors (RXRs) are crucial nuclear receptors involved in various physiological processes.
  • Selective modulators of RXRs are sought for therapeutic applications.
  • LG101506 is a known RXR selective modulator.

Purpose of the Study:

  • To synthesize novel fluorinated trienoic acid analogues of LG101506.
  • To evaluate the binding affinity of these analogues to RXRalpha.
  • To assess their efficacy in activating RXR homo- and heterodimers.

Main Methods:

  • Chemical synthesis of fluorinated trienoic acid analogues.
  • In vitro assays to measure binding to RXRalpha.
  • Functional assays to determine activation of RXR homo- and heterodimers.

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Main Results:

  • Synthesis of a series of fluorinated trienoic acid analogues was successful.
  • Binding and activation potency varied based on the position of fluorine atoms.
  • Certain analogues exhibited improved pharmacological profiles compared to the parent compound.

Conclusions:

  • Fluorination position is a critical determinant of RXR binding and activation.
  • Novel fluorinated analogues show potential as improved RXR modulators.
  • Further investigation into these compounds may yield new therapeutic agents.