| Literature DB >> 25790336 |
Sébastien L Degorce1,2, Andrew Bailey1, Rowena Callis3, Chris De Savi1, Richard Ducray2, Gillian Lamont1, Philip MacFaul1, Mickael Maudet2, Scott Martin1, Rémy Morgentin2, Richard A Norman3, Aurélien Peru2, Jennifer H Pink1, Patrick A Plé2, Bryan Roberts1, James S Scott1.
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.Entities:
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Year: 2015 PMID： 25790336 DOI： 10.1021/acs.jmedchem.5b00066
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446