Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.

Journal of Medicinal Chemistry
Sébastien L DegorceJames S Scott

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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Citations

May 8, 2016·European Journal of Medicinal Chemistry·Jyoti DandriyalVikas Jaitak
Nov 1, 2016·Breast Cancer : the Journal of the Japanese Breast Cancer Society·V L MaruthanilaJibon Kotoky
Jan 25, 2017·Journal of Medicinal Chemistry·Rui XiongGregory R J Thatcher
Feb 1, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Angela StefanachiAngelo Carotti
Jun 27, 2018·Journal of Enzyme Inhibition and Medicinal Chemistry·Ahmed SabtLaila A Rashed
Oct 13, 2016·Annual Review of Pharmacology and Toxicology·Daniel P Bondeson, Craig M Crews
Sep 12, 2020·ChemMedChem·Lucia Wang, Abhishek Sharma
Jan 15, 2019·Journal of Medicinal Chemistry·James S ScottRadoslaw Polanski

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