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Bioorg Med Chem Lett. 2006 Feb 15;16(4):821-4. Epub 2005 Nov 22.

Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.

Author information

1
Discovery Research, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.

Abstract

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.

PMID:
16307879
DOI:
10.1016/j.bmcl.2005.11.030
[Indexed for MEDLINE]
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