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.
MeSH terms
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Animals
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Brain / metabolism
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Dose-Response Relationship, Drug
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Drug Design
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Estrogens / blood
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Female
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Humans
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Leiomyoma / drug therapy*
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Models, Chemical
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Ovary / drug effects*
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Ovary / metabolism
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Rats
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Rats, Sprague-Dawley
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Selective Estrogen Receptor Modulators / chemistry
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Selective Estrogen Receptor Modulators / pharmacology*
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Software
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Structure-Activity Relationship
Substances
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Estrogens
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Selective Estrogen Receptor Modulators