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Bioorg Med Chem Lett. 2010 Jan 1;20(1):272-5. doi: 10.1016/j.bmcl.2009.10.111. Epub 2009 Nov 10.

Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.

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  • 1Environmental Health Science Laboratory, Sumitomo Chemical Co., Ltd, 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-8558, Japan.


The synthesis and SAR studies of 3- and 4-substituted 7-hydroxycoumarins as novel 17beta-HSD3 inhibitors are discussed. The most potent compounds from this series exhibited low nanomolar inhibitory activity with acceptable selectivity versus other 17beta-HSD isoenzymes and nuclear receptors.

Copyright 2009 Elsevier Ltd. All rights reserved.

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