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Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5.

Design and synthesis of fluorinated RXR modulators.

Author information

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

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.

PMID:
12951091
DOI:
10.1016/s0960-894x(03)00703-0
[Indexed for MEDLINE]

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