4.5 Article

Synthesis and identification of novel 11β-aryl-4′,5′-dihydrospiro[estra-4,9-diene-17β,4′-oxazole] analogs with dissociated antiprogesterone activities

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 21, Pages 5754-5757

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.08.064

Keywords

steroidal spiro-oxazole; progesterone receptor; glucocorticoid receptor; antagonist; selective progesterone receptor modulators

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A series of novel 11 beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17 beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486). (c) 2007 Elsevier Ltd. All rights reserved.

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