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Bioorg Med Chem Lett. 2007 Jul 1;17(13):3544-9. Epub 2007 Apr 24.

Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.

Author information

1
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. t_richardson@lilly.com <t_richardson@lilly.com>

Abstract

Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.

PMID:
17482463
DOI:
10.1016/j.bmcl.2007.04.044
[Indexed for MEDLINE]

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