Bioorganic & Medicinal Chemistry Letters 2010-01-01

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

Koichiro Harada, Hideki Kubo, Yoshitaka Tomigahara, Kazuhiko Nishioka, Junya Takahashi, Mio Momose, Shinichi Inoue, Atsuyuki Kojima

Index: Bioorg. Med. Chem. Lett. 20 , 272-5, (2010)

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Abstract

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.