Investigation Of (E)-344-(2-Oxo-3-Aryl-Chromen-4-Yl)Oxyphenyl]Acrylic Acids As Oral Selective Estrogen Receptor Down-Regulators
JOURNAL OF MEDICINAL CHEMISTRY(2015)
Abstract
A novel estrogen receptor down-regulator, 7-hydroxycoumarin (5, SS5020), has been reported with antitumor effects against chemically induced mammary tumors. Here, we report on our own investigation of 7-hydroxycoumarins as potential selective estrogen receptor down-regulators, which led us to the discovery of potent down-regulating antagonists, such as 33. Subsequent optimization and removal of the 7-hydroxy group led to coumarin 59, which had increased potency and improved rat bioavailability relative to SS5020.
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