Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
作者： Sébastien L. Degorce , Andrew Bailey , Rowena Callis , Chris De Savi , Richard Ducray
DOI: 10.1021/ACS.JMEDCHEM.5B00066
关键词:
摘要: 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 down-regulators, which led us to the discovery potent down-regulating antagonists, such 33. Subsequent optimization and removal 7-hydroxy group coumarin 59, had increased potency improved rat bioavailability relative SS5020.
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